5^th International Conference and Exhibition on Pharmaceutics & Novel Drug Delivery Systems March 16-18, 2015 Crowne Plaza, Dubai, UAE

Biography:

Dr. Vignesh Muthuvijayan has completed his PhD from the Department of Chemical Engineering, Oklahoma State University, USA and postdoctoral studies from Department of Biomedical Engineering, School of Medicine, Johns Hopkins University, USA. He is currently working as an Assistant Professor in the Department of Biotechnology, Indian Institute of Technology Madras. His research focuses on developing polymeric materials for biomedical applications such as implants, drug delivery and tissue engineering.

Abstract:

Liposomes have been used in drug delivery for decades. After drug loading, liposomes must be separated from the unloaded drug molecules. Currently, dialysis, density gradient centrifugation, ultracentrifugation and column chromatography are used for separation of liposomes. These techniques are primarily applicable for small-scale production 1. Also, they are tedious and/or expensive. Here, we have developed a rapid and cost-effective method for separation of liposomes from unloaded drug molecules. We prepared phospholipids from egg yolk 2 and prepared the liposomes using previously described techniques 3. We separated the liposomes using precipitation with ethanol, acetone and isopropanol. We optimized the separation process using a 2-factorial design with volume of precipitating agent and time as the input factors and percentage recovery and particle size ratio as the output factors. We considered the points with 100% recovery and particle size ratio of 1 as the optimum points. The studies showed that the volume of precipitating agent used plays a significant role separation of liposomes and not the time of incubation. We also identified that optimum separation was obtained using ethanol and acetone (Figure 1a and 1b). In case of isopropanol, although particle size wasn’t affected, the maximum recovery obtained was less than 60% (Figure 1c). The results show that using ethanol and acetone, we can separate liposomes within 20 minutes with a recovery close to 100% without change in particle size. TEM analysis has to be performed to confirm the results observed. A model drug (Toluidine Blue) was loaded to the separated liposomes and the release was studied (Figure 2). The release profiles were modeled using Higuchi’s equation, Peppas model and saturation kinetics model.

Biography:

Robert Pola has completed his PhD at the age of 29 years from Institute of Macromolecular Chemistry, Academy of Sciences of the Czech Republic (IMC). He is the member of Department of Biomedicinal Polymers of IMC. He has published 15 papers in reputed international journals.His research focus is based on synthesis of peptide sequences and preparation of water-soluble polymer conjugates used as drug delivery systems for effective treatment of cancer or for vaccination.

Abstract:

Conjugation of anti-tumor drugs to polymer carriers can improve their pharmacological properties. An attached tumor-targeting ligand further increases therapeutic efficiency. Oligopeptides are frequently used as targeting ligands mimicking determinant protein fragments. However, selective delivery to tumor cells is not the only requirement. An enhanced cellular uptake is another key factor for the therapeutic efficiency of the polymeric drugs. This can be mediated by cell-penetrating peptides (CPP) which facilitate the conjugate’s penetration through the cytoplasmic membrane. Yet another key issue is the controlled release of the cargo. We propose a new generation of polymer therapeutics targeted to tumor cells using specific targeting ligands and CPPs. The distinct advantage of this approach is that all components, i.e. drug, targeting ligand (RGD based peptides) and CPP (PFVYLI, R9F2, etc.), are attached to a polymer carrier based on a copolymer of N-(2-hydroxypropyl)-methacrylamide. A cytostatic drug pirarubicin attached to the polymer is inactive during the transport in the blood; once inside the cell it is released and regains its activity. The polymer conjugates with CPP exhibited much higher cell uptake than the control conjugates as shown by FACS and fluorescence confocal microscopy.

Biography:

Luisa, after a long post-doctoral experience at the University of Milan in the field of transport physiology with a specific competence in permeability processes through intact epithelia and cellular membranes, Dr.Fiandrais nowresearcher in L. Sacco University Hospital of Milan. Her present field of interest is the study of the delivery of nanoformulated in animal models for future application in breast cancer oncology and HIV treatment.From 2010, as scientific coordinator of the NanoMeDia Project, funded by RegioneLombardia (Italy), Dr.Fiandra coordinates the research activity of the Nanomedicine Laboratory of L. Sacco University Hospital, the NanoBioLab of the Department of Biotechnology and Biosciences (University of Milan-Bicocca) and the Center of Electron Microscopy for Nanotechnologies Appllied to Medicine of the Department of Biomedical and Clinical Sciences L. Sacco (University of Milan).

Abstract:

In HIV management, eradication of virus by sanctuary sites remains a main challenge. In fact, although current antiretroviral (ARV) therapies suppress plasma HIV below detectable levels in a consistent proportion of subjects, total virus eradication is still beyond our possibilities. An important barrier to achieve such goal is related to the suboptimal concentrations of ARVs within the HIV sanctuaries. Th e central nervous system (CNS) is a key example of sanctuary where viral replication occurs despite of a complete viral suppression in the peripheral blood. In recent years, nanotechnology has provided great promise in the eradication of HIV from CNS. However, this is the first time in which a complex and heavy peptide like enfuvirtide (Enf), which normally does not penetrate in the CNS, is found to cross the blood brain barrier (BBB) of mice, by conjugation with a nanoconstruct. We demonstrated that iron oxide nanoparticles coated with an amphiphilic polimer (MYTS), labeled with FITC, increased AF660-Enf translocation across BBB in vitro, using a validated BBB model composed of rat BMVECs and astrocytes, and in mice i.v. injected with the nanoformulated Enf. We describe a delivery mechanism involving the uptake of MYTS-Enf in the endothelial cells, the nanocomplex dissociation and the release of the peptide, which is effi ciently excreted into the outside environment (Figure 1). Th e dissociation seems to involve the degradation of the PMA shells bearing the peptide into the more mature endosomal compartments, as an eff ect of the increased acidity and enzymatic activity of their inner environment, to be then completed within lysosomes.

Biography:

Alena Braunová has completed her PhD in 2006 from Institute of Macromolecular Chemistry, Academy of Sciences of the Czech Republic (IMC). She is a member of Department of Biomedicinal Polymers of IMC. She has published 12 papers in reputed international journals, which were cited more than 60 times and she is an author of more than 40 international conference contributions and abstracts.Her research focus is based on preparation of micellar and water-soluble drug delivery systems for effective treatment of cancer and cancerdiagnostics.

Abstract:

Tumour cell resistance tomultiple cytotoxic drugs (multi-drug resistance, MDR), especially to anthracycline antibiotics, is one of the main causes of imperfect efficacy of chemotherapy in current medicine. MDR is a protective response of tumour cells caused by long-term effect of drugs onto the cells. The cells could then decrease the drug intracellular concentration by various mechanisms – e.g. by drug effluxusing special transmembrane proteins, particularly P-glycoprotein (P-gp). P-gp is an ATP-dependent efflux pump of xenobiotic compounds with wide substrate specificity and it is a member of a family of ATP-binding cassette transporters. While in healthy cells P-gp effluxes xenobiotics and toxins, in tumour cells, where P-gp is expressed in much higher amount, contributes P-gp due to this property frequently to MDR. Therefore, P-gp inhibition should cause a better drug penetration into the cells, and thus more effective cancer therapy. Our work is focused on the synthesis of amphiphilic block polymer-drug conjugates, where one block is based on hydrophilic poly(N-2-hydroxypropyl methacrylamide and the other is hydrophobic derivative of poly (propylene glycol), which should be responsible for P-gp inhibition. These blocks form particles due to their different physico-chemical properties and thereby polymer-drug-conjugate molecular weight increase. This fact should be an advantage for passive targeting of these systems preferentially into solid tumours due to the Enhanced Permeability and Retention effect. The drug doxorubicin is bounded to the conjugate by pH-sensitive hydrazone bond, good degradable inside the cells (pH 5.0) but more stable in bloodstream (pH 7.4). Cell viability assay on MDR cancer cell lines are under way.

Biography:

Tsann-Long Su has completed his PhD from the Free University of Berlin, and then worked as a Postdoctoral Fellow at Schering AG, Berlin, Germany. He then moved to the Memorial Sloan-Kettering Cancer Center, New York, USA, and continued his research on developing antiviral and anticancer agents. Currently, he is working as a Research Fellow at the Institute of Biomedical Sciences, Academia Sinica, Taipei, Taiwan. His research interests include anticancer drug design and synthesis, pharmacology and phytochemistry.

Abstract:

Lung cancer causes one third of death from cancer worldwide. In clinical, surgery, radiation therapy, chemotherapy, and targeted therapy are commonly used for the treatment of the malignancy. However, the success of these agents is limited due to the emerging of drug resistance. Th ereby, there is an urgent need to discover novel agents with improved efficacy and safety profiles for the treatment of lung cancers. We have recently synthesized a series of indolizino[6,7-b]indoles, which were designed as a hybrid molecule containing biologically active β-carboline (topoisomerase I and II inhibitory moiety) and bis (hydroxymethyl) pyrrole (DNA cross-linking moiety) for antitumor studies. Of these derivatives, we found that BO-1978 exhibited potent therapeutic efficacy against various non-small-cell lung carcinoma (NSCLC) cells both in vitro and in the tumor xenograft or orthotopic models. Remarkably, we found that the combination treatment of BO-1978 with gefitinib has enhanced efficacy against EGFR-mutated NSCLC and was superior to that of gefi tinib or cisplatin alone in tumor bearing mice. Moreover, this hybrid molecule displayed topoisomerases I and II inhibitory eff ects and induced DNA interstrand crosslinking. The studies on the toxicity/safety in mice revealed that this agent has low toxicity to the host; no major pathology or blood biochemistry changes. We also demonstrated that BO-1978 has good pharmacokinetic (PK) profile in animal. These findings indicated that BO-1978 can be selected as a candidate for preclinical study, IND application, and eventually for clinical trial for the treatment of NSCLC patient.

Biography:

Hudson Polonini, pharmacist, has completed his PhD at 2014 from Federal University of Juiz de Fora and currently performs postdoctoral studies from Federal University of Santa Catarina. He studies: analysis and control of medicines and related products, pharmaceutical and cosmeceutical technology, biopharmacy, natural products and ecotoxicology. He has published 30 papers in reputed journals and he has two patents, and he also has some awards in innovation competitions.

Abstract:

Resveratrol (3,5,4-trihydroxystilbene) is a prominent substance in currently pharmaceutical research. It is a naturally occurring non-flavanoid phenolic compound produced by some spermatophytes, notably grapes (reason why it is found in high concentrations in many red grape skins and their wines). The trans-resveratrol isomer is more biologically active: it has been reported to possess antioxidant, neuroprotective, antiphotoaging and antiviral activities, and it also seems to play a role in the prevention and reduction of pathological processes such as inflammation, cancer and heart diseases. However, trans-resveratrol has poor oral bioavailability, which creates a dilemma between its great in vitro efficacy and its low in vivo effect, mainly because it is extensively metabolized in the body. Our group has been dealing with this question. Two previous published studies on its permeations through excised human skin showed that this can be a good alternative to avoid the oral route. They used different methods and obtained very similar results of permeation percentage from emulsions (62.6 % using retention mapping and 64.9% using tape stripping). Another strategies that are currently under evaluation in our laboratory is the transmucosal route, either by oral or vaginal mucosal. Our preliminary results show that these seem to be also efficient routes, as they can act both for systemic drug delivery as for local clinical conditions. Finally, the inclusion of trans-resveratrol in solid lipid nanoparticles (SLN) is will offer additional advantages of stability and delivery of the substance to the body, as shown by the results obtained until now. In addition, toxicology studies are been run in parallel. These data altogether show that these alternative strategies can be safe and of clinical relevance for a more efficient delivery of resveratrol to humans.Thus, transdermal or transmucosal delivery of resveratrol is paramount for the effective insertion of the substance into pharmaceuticals for clinical practice.

Biography:

Malihe is a second year PhD student in the Experimental Medicine Program under the supervision of Dr. Aziz Ghahary. She has joined the Burn & Wound Healing Laboratory in January 2011 after obtaining her Masters degree in Biotechnology form University of Tehran, Iran. Malihe’s project focuses on incorporating anti-fibrotic drugs into nanofibers in order to develop novel bioactive wound care products to treat dermal fibrosis. Malihe has expertise in protein purification and characterization, monoclonal and polyclonal antibody production and characterization, PCR, Western blotting and cell culture. In her free time, Malihe is volunteering as the president of Canadian Biomaterial Society student chapter. She also enjoys painting and outdoor activities.

Abstract:

Wound healing outcome is regulated by a fine balance between deposition and degradation of extracellular matrix (ECM). Over healing process in skin is mediated by exaggerated ECM deposition and abnormalities in ECM degradation. Moving toward novel approaches to prevent skin fibrosis, we identified a small molecule having anti-scarring properties which is called Fibrosis Stop 2 (FS2). Although daily application of FS2 containing cream eliminates evidence of scarring in a fibrotic rabbit ear model, an effective wound dressing, releasing controlled doses of FS2, will be more beneficial for FS2 delivery to extensive burns where the wound dressing get changed every 4-5 days. This study aims to develop novel biomedicated electrospun nanofibrouse mats for controlled delivery of FS2, directly to an injury site to improve the wound healing outcome. Nanofibers of Poly (methyl methacrylate) and different composite blends of Poly (methyl methacrylate)/Poly (ethylene glycol) with FS2, were successfully electrospun for the first time. Scanning electron microscopy was performed to determine the morphology and average diameter of the electrospunnanofibers. In vitro drug release evaluations showed that addition of PEG to PMMA has a proportional enhancing effect on the release of FS2 from nanofibrouse mats. While FS2-loaded PMMA/5% PEG mats showed significantly lower levels of burst release and prolonged release up to 5 days, medicated PMMA/20% PEG mats demonstrated complete drug release within 24 hours. The biological activity of the nanofiber incorporated FS2 was evaluated in vitro by determining the effect of these dressings on ECM components’ expression by fibroblasts. These studies showed that nanofiber incorporated FS2 significantly decreases the expression of collagen-I and α-smooth muscle actin and increases the expression of MMP1 which indicate the preservation of FS2 biological activity during the electrospinning process. Electrospinning of PMMA/PEG blend exhibited a useful and convenient method for controlling the rate and period of FS2 release in wound healing applications. The findings of this study confirmed that it is feasible to develop an anti-fibrogenic dressing for prevention of dermal fibrosis frequently seen upon burn, deep trauma and surgical procedures.

Biography:

Nivorozhkin is an entrepreneur and a team builder in life sciences’ arena with vast experience and track record in an early technology transfer and development. He was a co-founding member of Boston BioCom, LLC, a biopharma company funded by the seed investment from Pfi zer. Alex gained substantial experience in the commercial aspects of drug discovery and development at Epix Medical and Inotek Pharmaceuticals where he served as the company’s Head of Medicinal Chemistry. He served as a Senior Program Manager at the Center of Integration of Medicine and Innovative Technologies (CIMIT) at Massachusetts General Hospital, a consortium of the Harvard Medical School-affliated hospitals, Boston University, Draper Laboratory and MIT aimed at developing new medical devices; and a Scientific Programs Officer at Sheldon and Miriam Adelson Medical Research Foundation. He is a co-inventor of several drug candidates that have advanced to clinical trials and late pre-clinical studies in the United States, has co-authored over 60 scientific publications in different areas of chemistry, chemical biology, and material sciences and holds more than 20 patents. Alex received a PhD in Physical Organic Chemistry from Rostov University and conducted the postdoctoral research at the University Paris-Sud, France, and the Department of Chemistry and Chemical Biology, Harvard University, Cambridge.

Abstract:

Sol-gel-derived and silica-containing materials have made significant strides into the material sciences’ applications and established presence in multiple commercial products and industrial technologies. In biomedical field, extensive researchindicated their potential utility in areas such as enzyme and live-cell encapsulation. These materials hold promise in a drug delivery area as well. General biocompatibility and biodegradable properties make silicas and sol-gels attractive matrixes. Nanotechnology brings in a possibility for a subtle tune-up of the particles fine structure and variety of functionalization opportunities for covalent and non-covalent binding of the cargo. This presentation will review key developments in using silica materials in drug delivery applications and focus on the properties and processes that could be controlling issues in moving early discovery findings into the realm of commercial applications and platform technologies that are compatible with FDA requirements for drug products to enter clinical trials.

Biography:

Dr. Wu is currently a Professor and the Vice Director of the Institute of Cellular and Organismic Biology at Academia Sinica. He is also a Professor at the College of Medicine of the National Taiwan University. His research interest focuses on the development of targeting drug delivery systems for cancer therapy and targeting imaging. He has also developed phage display and affinity maturation methods to generate of fully human monoclonal antibodies for treatment of human diseases. Dr. Wu is actively involved in basic and translational research in the areas of oncology and has received numerous awards.

Abstract:

Lack of tumor specificity remains a major problem for chemotherapies in which side effects prevent the delivery of the drug dosages needed to eliminate the majority of cancer cells. Recently, we developed phage display methods to identify several novel peptides and human single chain variable fragment (scFv) antibodies that bind specifically to the plasma membrane of cancer cells. In an effort to develop targeting drug delivery systems, we used peptide-linked liposomes that carried doxorubicin to treat severe combined immunodeficiency (SCID) mice bearing human tumor xenografts. The peptide-functionalised liposomes were found to have an enhanced anti-tumor effect and reduced toxicity. Combination treatment of peptide-mediated targeting liposomes was able to completely eradicate tumors in three-sixth of the total number of tumor-bearing mice without any signs of recurrence. Targeting liposomes improved the therapeutic index by enhancing therapeutic efficacy, reducing side effects, and increasing the survival rate of tumor-bearing mice in orthotopic animal model. The tumor site fluorescent intensity in the mice treated with targeting peptide-linked quantum dots showed higher tumor uptake and increased tumor-normal tissue ratios. In addition, in vivo imaging by scFv-conjugated quantum dots clearly demonstrated the potential clinical use of the scFv in tumor targeting and imaging. Ligand-conjugated liposomes enhance pharmacokinetic and pharmacodynamic properties, improve efficacy and safety profiles, and allows for controlled biodistribution and drug release. Our study indicates that peptide- or scFv-mediated drug delivery systems show great promise for their applications in tumor-targeted drug delivery and imaging.

Biography:

Khaled Hosny: Associate Professor of Pharmaceutics and Industrial Pharmacy at King Abdulaziz University, Saudi Arabia. He was granted his PhD from Cairo university, Egypt, in 2006. He is currently supervising 3 PhD & 8 Master degree postgraduate students. Dr. Hosny participated in the advanced research projects. Major research interests focused on Novel drug delivery systems. Dr. Hosny has a lot of publications in international journals.

Abstract:

Objective: The aim of this research was to utilize nanotechnology for oral alendronate sodium delivery, wherein ALS is incorporated within an enteric coated solid lipid nanoparticles (EC-SLNs). The putative advantages are enhancing the absorption and bioavailability, controlling the release, and preventing the free ALS from coming in direct contact with the GI mucosa thereby reducing the possibility of side effects.

Methods: (EC-SLNs) were prepared by a modified solvent emulsification-evaporation method based on a w/o/w double emulsion technique, effect of different process variables as solid lipid type, surfactant type and concentration, addition of charge inducing agent, enteric coating with Eudragit S100, and ultrasonication time on the particle size, zeta potential, entrapment efficiency, release in acidic and basic media were evaluated. Pharmacokinetic were conducted on rabbits

Results: EC-SLNs were successfully prepared with paricle size 74 nm, zeta potential 36 mV, and entrapment efficiency 56%. The nanoparticles released ALS only at pH 7.4 which ensure the efficiency of enteric coating. The bioavailability enhanced by more than 14 fold in rabbits.

Conclusion: EC-SLNs is a promising formula for the delivery of ALS, eliminating its oesophageal side effects, and enhancing its bioavailability.

Biography:

Min Zhao completed her Ph.D from the School of Pharmacy, University of East Anglia, UK in 2010 and became a Lecturer in Pharmaceutics in the School afterwards. In 2013, Min joined the School of Pharmacy, University College London (UCL) and her main research focus has been on amorphous solid dispersion (ASD) technology as a means of improving the bioavailability of poorly water soluble drugs. Min’s talk on “Overcoming Devitrification of a Low Tg Drug by Spray Drying as a Solid Dispersion” has won the ‘Best Presentation Award’ at Amorphous III Conference run by the Academy of Pharmaceutical Sciences (APS).

Abstract:

Drug-polymer interaction and anti-plasticizing effect of the polymer are the two well-known mechanisms under which amorphous drugs may be generated and stabilized within solid dispersions. In this study, we deliberately select polymers which in the previous studies showed insignificant interactions with the drug of interest with a view to better understanding other factors determining the enhanced stability. Firstly, long term studies were performed under different stability conditions with a number of fully amorphous solid dispersions at varying polymer grades and drug loadings. The inhibition effect on morphologic change and water uptake appeared to be the key explanations for the stabilizing effects of polymers, varying with formulation and storage condition. In particular, PVP K29/32 was more effective for high temperature stability through sustaining the particle morphology while Plasdone S630 showed better stability over high humidity storage. Water uptake issue was further improved via incorporating zein (a class of prolamine protein) into the latter system. It was found that the binary system showed amorphous-amorphous phase separation while the ternary system remained stable through the entire testing period, indicating a significant inhibiting effect of zein on the water uptake of amorphous solid dispersions. Interestingly, the water induced amorphous-amorphous phase separation was well monitored using Transition Temperature Microscope (a novel method of nano-thermal analysis), which was supported by Differential Scanning Calorimetry and Scanning Electron Microscope techniques. In terms of the relationship between stability and dissolution performance, the occurrence of morphologic change and phase separation did not show profound effects on the drug release profiles.

Biography:

Mine Orlu Gul is a pharmacist. She graduated from Istanbul University, Faculty of Pharmacy. She received her MSc on the subject of colon targeted microspheres in 2003, followed by a PhD about fl uorescently-labeled nanoparticles and their interaction with lung cells in 2008 from Istanbul University, Faculty of Pharmacy. During her PhD studies, she held a 1-year visiting scientist post at King`s College London funded by Marie Curie Host Fellowship for Early Stage Training in the 6th Framework Programme of the European Commission. She started The School of Pharmacy, University of London in March 2008 as a post-doc for Prof Oya Alpar to perform studies on vaccine formulations. In her second post-doc position, she joined Dr Catherine Tuleu`s group as a Teaching and Research Fellow at UCL School of Pharmacy, Department of Pharmaceutics, Centre for Paediatric Pharmacy Research to work in the fi eld of paediatric pharmaceutics and drug delivery. Her fellowship was funded by UK NIHR Medicines for Children Research Network (MCRN) from June 2009 to September 2012. She was appointed as Lecturer in Pharmaceutics to develop a research agenda in geriatric pharmaceutics in October 2012. She is a member of UCL Grand Challenges of Human Wellbeing Executive Group and Geriatric Medicines Society Age Appropriate Formulations Working Group. She also co-chairs The Academy of Pharmaceutical Sciences-Age Related Medicines Focus Group.

Abstract:

The current patient-centric formulation development specifi cally for geriatric patients is limited. However, steps are taken to improve the present status. Th e European Medicines Agency`s Geriatric Medicines Strategy, FDA`s Guidance of Industry E7 Studies in Support of Special Populations: Geriatrics - Questions and Answers document and EFPIA Position Paper on Drug Development for Older and Ageing Patients are promising to increase the availability of medicines tailored for needs of older patients. Th e review of current scientifi c literature shows that further research should be performed to rationalize formulation development for elderly. Besides the conventional biopharmaceutical properties of the drug and quality aspects of the formulation, organoleptic properties such as ease of swallowing, taste and simplicity of opening packaging should be considered at early stage of product development due the potential impact on patient acceptability. The presentation will cover several ongoing scientific studies to explore the pharmaceutical needs and solutions under the light of the opinion of older people obtained during public engagement workshops.

Biography:

Rajiv Dahiya is Doctor of Science in Clinical Pharmacology from International University for complementary Medicine, Colombo, Sri Lanka and Ph.D in Pharmacy from Uttar Pradesh Technical University, Lucknow, Uttar Pradesh), India. He is presently President of Association of Pharmacy Professionals (APP), editor-in-chief of international level journal - Bulletin of Pharmaceutical Research (BPR) and Principal at Globus College of Pharmacy, Bhopal, Madhya Pradesh, India. He has 13 years of teaching and 10 years of research experience. His research area is synthetic peptide chemistry and uptil now, he has published 50 research papers and 9 review articles in various international and national journals covering a total impact factor of 36.6. Dr. Dahiya is recipient of ‘Innovative Research Award’ in Jun 2012, ‘Excellence Award’ in Pharmacy in Feb 2014, ‘Young Pharmacist Award’ & ‘Young Scientist Award’ in Mar 2014.

Abstract:

Marine sponges and higher plants are enriched with several active constituents responsible for their biopotency. Among these, peptides have received special attention due to their wide biological profile including antimicrobial, anti-inflammatory, anti-AIDS, antimalarial, cytotoxicity, nematocidal, inhibitory activity against thrombin, trypsin, plasmin, tyrosinase and superoxide generation, calcium channel antagonistic activity and may prove better candidates to overcome the problem of resistance towards conventional drugs. Although linear peptides are associated with diverse bioactivities but cyclopolypeptides dominate over them due to the fact that inherent flexibility of linear peptides lead to different conformations which can bind to more than one receptor molecules, resulting in undesirable adverse effects. Furthermore, cyclization of peptides reduces the degree of freedom for each constituent within the ring and thus substantially leads to reduced flexibility, increased potency and selectivity of cyclic peptides. These cyclic congeners possess unusual or modified amino acid residues like Dhha, Adha, Ahoa, AHMP and exhibit their bioactivities through binding to corresponding enzymes. This characteristic feature can allow bioactive cyclopeptides to act as therapeutic agents in this resistant world. In order to design and develop long-acting, more effective peptide/protein drugs, the controlled release mechanisms and effective parameters need to be understood. Various peptide/protein delivery systems includes biodegradable and nondegradable microspheres, microcapsules, nanocapsules, injectable implants, diffusion-controlled hydrogels and other hydrophilic systems, microemulsions and multiple emulsions, and the use of iontophoresis or electroporation etc. Controlled delivery of peptide and protein drugs provides improved efficiency, reduced toxicity and improved patient convenience in addition to maximum stability, activity and bioavailability.

Biography:

Abstract:

Guar also known as cluster bean is the source of a natural hydrocolloid which is cold water soluble and form thick solution at low concentrations. Owing to new technology, research and development being done in this field, the natural gum property has found varied applications from food to pharmaceutical industry. Due to its fascinating properties it is used as a rheological modifier. Guar gum can be modified by derivatization, grafting and network formation to alter its properties and make it suitable for biomedical applications. In order to enhance its applicability in the industries, its derivatization can be carried out to get novel derivatives with desired properties. Therapeutically it is used as hypoglycemic, hypolipidemic, antimicrobial, antiproliferative, appetite suppressant, bulk forming laxative in collitis and crohn's disease. The swelling property of guar gum is of importance in managing the drug release rate in innovative pharmaceuticals. The present talk is a review highlighting the total over-view from the plant to production to the application of this wonderful herb and its potential as a carrier for targeted drug delivery systems.

Biography:

Sandeep Arora carries an impressive professional experience spanning 21 years—3.5 years in pharma production and quality assurance in Glaxo, Blue cross and 17.5 years in teaching/training and research—in the fi elds of pharmacognosy and natural products, regulatory affairs, industrial pharmacy, and management. He is the author of the book titled, “Pharmaceuticals – Issues for Industrial Management”; has been the honorary editor of “Advanced Drug Review”—a quarterly drug pharmacology review index—since 2005; and has to his credit about 50 national and international publications. His area of specialization and research are medicinal natural products (phytochemical, pharmacological evaluation and standardization), development and regulatory aspects of herbal and other products, and industrial management. Under his capable guidance two PhD students have completed their theses; 15 M. Pharm. students have completed their theses; and eight Ph D projects are currently being guided by him.

Abstract:

Herbal ZnO nanoparticles were synthesized using Asparagus root extract via co precipitation methods. Th e synthesized nanostructures were characterized by XRD, SEM and TEM which reveal the formation of crystalline ZnO nano-structures and spherical and granular nature with characteristic peaks of ZnO nanoparticles. Th e nanoparticles of Zinc and extract were also standardized for herbal marker component and Zinc and then tablet formulations were developed and standardized for formulation parameters. It was observed that the nanoparticles off ered a spherical and granular nature, which off ered very convenient advantage by producing very good preformulation characters including fl ow and particle size as compared to taking dry herbal powder as such which produce great diffi culty in tableting. Th e formulated tablets were standardized for formulation parameters on the basis of evaluation characteristics including disintegration time, dissolution time, friability and content for use as herbal nutraceuticals tablets and further development using various extracts.

Biography:

Chemical Engineering degree. Involved in Clean Room technologies since 1980. At present he is in charge of the Integrated Projects Business Unit at Fedegari Group, dealing with the design and the supply of new solutions for the sterile drug manufacturing including GMP robotics. Scientific Technical Association activities: member of the board of the Italian association of contamination control ASCCA (www.ascca.net) since 1986, President of ASCCA 1998-2000, ISPE member since 2001. At present ASCCA vice president. Promoter and responsible of the training course on “General introduction on Clean Room technology, isolation concepts and critical parameters definition”. Trainer on pharmaceutical HVAC design at La Sapienza University (Roma) for students of chemical and pharmaceutical technology. Author of several papers on clean technologies and experienced giving training lectures to AIFA GMP Italian inspectors.

Abstract:

One of the most problematic issues of the aseptic manufacturing is the involvement of the personnel. Human being is generating every minute million of particles and some of them are biologically active and might generate a product contamination. Now the technology can help us in removing from the aseptic manufacturing equation the human being and the relevant impact in the sterility of the product. Stainless Steel GMP robotic arms have been introduced to handle fill finish operation within a gloveless isolator. The advantage of this solution, apart from sterility improvement, is the possibility to handle High Potent Active Pharmaceutical Ingredients (HPAPI) like cytotoxic drugs. The presentation will go through all the main features of this gloveless robotic solution.

Biography:

Husam Younes is a graduate of the Faculty of Pharmaceutical Sciences at the University of Alberta (UA) in Edmonton, Alberta, Canada. He received his BSc (Pharm) in 1992 followed by MSc (Pharmaceutical Technology) in 1995. He worked as a Technical Manager in the Pharmaceutical Industry in Palestine and Jordan then completed his PhD from UA in 2002. In August 2007, Younes moved to Qatar to start his new career as the Founding Chair of Pharmaceutical Sciences department in the new Pharmacy Program at Qatar University. He is currently an Associate Professor of Biopharmaceutics at the College of Pharmacy and the founder of the new Pharmaceutics and Polymeric Drug Delivery Research Laboratory. He previously worked in the pharmaceutical industry and also as a senior consultant to Newfoundland Health Department in Canada. His main research is in the areas of controlled drug release, biomaterials, tissue engineering and synthesis of novel biodegradable polymers designed for localized and targeted delivery of therapeutic proteins in cancer therapy. Younes supervised graduate students and postdoctoral fellows in his lab and acted as an editorial board member and a reviewer for many pharmaceutical and drug delivery journals.

Abstract:

Purpose: To formulate and evaluate oral dosage forms of Metformin hydrochloride (MH) having sustained-release properties that would also increase MH bioavailability and address the shortcomings in the currently marketed sustained release tablets.

Methods: MH micronized powder was dispersed in molten polymeric matrices composed of Gelucire® 50/13 and various proportions of high molecular weight hydrophilic polymers, hydrophobic oily semisolid excipients, and mucoadhesive polymeric materials. The MH loaded matrices were filled in hard gelatin capsules (HGC) each containing 500 mg MH and were subsequently characterized using Differential Scanning Calorimetry (DSC) and X-Ray Diff raction Analysis (XRD). The prepared HGC were subjected to content uniformity and in vitro dissolution testing according to the USP-35 compendial requirements. The dissolution data were compared to instant and sustained-release marketed tablets. Th e effect of incorporating various proportions of the semisolid excipients on MH dissolution release rate, were also investigated.

Results: MH content of the prepared HGC ranged between 96 to 103%. All the prepared semisolid fi lled HGC resulted in extended release profiles of MH that lasted between 5 to 11 hours and demonstrated a release pattern which typically follows the release from mixes of triglycerides with polyethylene glycol esters of fatty acids. Th e incorporation of muco-adhesive excipients like Carbomer to the Gelucire® 50/13-MH semisolid matrices extended the release of MH from 5 hours initially to 9 hours as a result of the formation of a gel layer around the matrix. However, the incorporation of diff erent hydrophilic excipients like PEG35000 and Gelucire® 44/14 along with the muco-adhesive excipients sustained the release of MH up to 11 hours. XRD analysis of the MH prepared matrices demonstrated minor changes in the crystalline nature of MH. Depending on the loading ratios and the nature of the semisolid matrices used, DSC analysis revealed the changes in MH crystallinity to be from 100 to 23 %.

Conclusion: HGC formulated using semisolid matrices showed promising results in extending the release of MH. However, bioavailability studies to test the ability of such Gelucire based HGC of MH to improve its bioavailability and in vivo residence times are future plans.

Acknowledgements: This work was made possible by a NPRP award [NPRP 09-795-3-215] to HM Younes from the Qatar National Research Fund (a member of The Qatar Foundation). The statements made herein are solely the responsibility of the authors.

Biography:

NaglaaG.Ahmed is a Associate Professor, Pharmaceutical Chemistry and Natural products Department, Dubai Pharmacy College, Dubai, UAE. She graduated from Faculty of Pharmacy, Cairo University, Egypt and received the PhD from the same college. She is a member in American society of Pharmacognosyand in Italo-Latin American Society of Ethnomedicine and as editorial board member in Natural Products Chemistry and research. Also she is a reviewer for many international Journals concerning chemistry and biological activity of medicinal plants. She published at least 30 scientific papers also contribute in publication of scientific book and her interest field is in bioactivity of medicinal plants.

Abstract:

Introduction: Liver diseases are considered as one of the serious health problems, as it is an important organ for the detoxification and deposition of endogenous and exogenous substances. A number of pharmacological and chemical agents act as hepatotoxins and produce a variety of liver ailments. Steroids, vaccines and antiviral drugs which have been employed as a therapy for liver diseases, have potential adverse effects especially when administered for long terms.Traditional healing practices are nowwidespreadamongst about 80% of the developed countries population and often termed alternative or complementary medicine. Aim:In the absence of reliable liver-protective drugs in modern medicine, hepatoprotective drugs from plant sources seem to have attractive alternatives.The aim of thisscientific lectureis designed to focus in the medicinal plants as well as the other alternative medicines which can be used as hepatoprotective and antihepatotoxic agent. Methodology: MedicinalPlants that are found in the Arabic Gulf, India and United State of America with scientific researches will be discussed in this lecture. The active constituents, mechanism of actions, safety, side effects and the contraindication of each plant will bediscussed as well. Other alternative medicines like aromatherapy, acupuncture therapy, breathing therapy and relaxation therapy will be deliberated. Those are found to be effective therapies in the protection of liver from many diseases.

Biography:

Abstract:

Osteoarthritis (OA) is among the most prevalent chronic human health disorders and the most common form of arthritis. It is among the leading cause of disability worldwide and with increasing life expectancy; OA is a major socioeconomic and clinical concern.OA is characterized by cartilage deterioration/damage, infl ammation, synovial fi brosis, subchondral bone remodelling and osteophyte formation. Aetiology and pathogenesisunderlying OA is poorly understood. Several preclinical animal models (large and small animal models) have been used to understand the mechanisms associated with the pathophysiology of OA disease. Further, several models serve as an essential tool to determine drug bio-distribution, activity, safety as well as the therapeutic eff ects at pre-clinical phase. In my talk, I will shed light on the usefulness and limitations of using small animal models of osteoarthritis in understanding (a) mechanisms of disease as well as in (b) drug delivery, biodistribution, activity, safety and therapeutic eff ects.

Biography:

Rob Schultheis is a President for ZebraSci/Mantis Vision Systems, USA. He completed his Master of Science (MS) and BS, Mechanical Engineering from Drexel University.

Abstract:

Autoinjector device performance is greatly impacted by primary container quality. In order to ensure a robust design, a thorough forensic analysis of all variables need to be understood as they eff ect performance. From this understanding specifi cations can be derived in order to ensure a successful injection every time. Th is presentation outlines how to practically observe variation in primary packaging as it relates to device performance and then links this gained knowledge to how to derive a robust specifi cation.

Biography:

B. B. Barik has completed his PhD in 1993 from Jadavpur University, Kolkata, India. He is the Professor in the department of Pharmaceutics, College of Pharmacy, Jazan University, Kingdom of Saudi Arabia. Earlier he worked as professor and head in the Univ Dept of Pharm Sci, Utkal University, Bhubaneswar, India and College of Pharmaceutical Sci, Berhampur, Odisha. He has published more than 50 papers in reputed journals and presented more than 100 papers in national and international conferences. He is serving as reviewer and editorial board member of reputed journals.

Abstract:

Antibiotic resistance is one of the major health problems worldwide. Resistance to penicillin is well recognized in Staphylococcus aureus and Staphylococcus epidermidis. During last decade various resistance mechanisms such as decreased uptake, increased effl ux of drug from bacterial cell, formation of biofi lms to avoid contact with antibiotics have been identifi ed that lead to failure in the treatment. Th e concept of drug delivery system is rapidly moving towards the development of biodegradable polymeric nanoparticles. For past two decades many researchers have been developing nanoparticle drug delivery especially delivering of anticancer drugs and vaccines. Th e main advantage of this system is to deliver drug moiety at the site of cell that can improve pharmacokinetic and pharmacodynamic profi les of the drug. Th us the nanoparticles improve solubility, stability and bioavailability of various drugs. However, it is limited by toxic profi le. Th erefore, nanoparticle drug delivery system is highly challengeable for researchers to overcome toxicity. Th e application of nanoparticle in the fi eld of Medicine and Pharmaceuticals will be exposed more and more in near future. In our study, the antibacterial effi cacy of penicillin loaded chitosan nanoparticles was evaluated against selected bacterial strains namely Staphylococcus aureus, Streptococcus pyogenes, Bacillus subtilis, Escherichia coli and Klebsiella planticola of clinical origin. Th e study suggested that penicillin nanoparticles showed better antibiotic delivery system than conventional penicillin. However, the study is still under process in order to overcome lacunae that we experienced in our earlier studies.

Biography:

Nawal Khalafallah Current research interests include improving drug performance using lipid vesicles as carriers. Industry-related research interests include looking at the effect of source of excipients on excipient characteristics, and on product performance. Participated in developing a postgraduate two year PharmD program for hospital pharmacists

Abstract:

Several published articles have tackled the issue of improving vancomycin performance. Th e performance areas targeted in these studies included broadening antibacterial spectrum to include Gram-negative organisms, enhancing antibacterial activity against drug resistant Staphylococcus aureus and enhancing the antibiofi lm activity. One of the active research areas in the Department of Pharmaceutics has been lipid vesicles including liposomes and niosomes among other types of modifi ed liposomes such as propylene glycol liposomes with the aim of using these vesicles as vancomycin carriers to improve antibiofi lm activity including inhibition and eradication of biofi lms forming on abiotic sufaces such as catheters. Th is presentation focuses on challenges encountered, and on lessons learnt, while conducting research in this area. Some of the challenges are related to vancomycin itself and some arise from the methodology used. Th e presentation also touches on speculation of how to move such systems from bench to bedside.

Biography:

Ruchi Chawla is an Assistant Professor at Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi. She has 6 years of teaching and research experience. Her areas of research are anti-microbial chemotherapy, nanotechnology and herbal drug delivery. She has a strong academic background and has published papers in reputed journals. She is also serving as an Editorial Board Member.

Abstract:

Solid lipid nanoparticles of curcumin (C-SLNs) were prepared using stearic acid as lipid carrier by nano precipitation technique and characterized for their physio-chemical properties. SLNs were incorporated in hydro gels prepared from Carbopol®934 and the eff ect of method of incorporation of SLNs on the hydrogel properties was studied by Texture Analyzer. For the purpose of study, three types of hydro gels were prepared, i) Blank hydro gels B1, B2 and B3 containing respectively 0.5, 1.0 and 2.0 % w/v carpobol; ii) In-situ hydro gels Y1, Y2 and Y3 by adding carbopol (0.5, 1.0 and 2.0 % w/v) to fi xed volume of C-SLNs suspension and; iii) Enriched hydro gels by mixing C-SLNs and blank carbopol (1% w/v) hydrogel in the ratios 1:1 (D1) and 1:2 (D2). C-SLNs exhibited a mean particle size of 527.6 nm, poly dispersity of 0.383 and 82.73% entrapment efficiency. In-situ hydro gels exhibited a concentration (carbopol) dependent increase in fi rmness, consistency, cohesiveness and viscosity, however, presence of C-SLNs signifi cantly decreased (p<0.05) these values in comparison to blank hydro gels. Similar observations were made in enriched hydro gels. Also, a signifi cant difference (p<0.05) in hydrogel properties was observed between in-situ and enriched hydro gels. It indicates that SLNs have an eff ect on the swelling properties of Carbopol. Occlusive properties of in-situ hydrogels were better than enriched and blank hydro gels. In-situ hydro gels also exhibited uniform and extended release of curcumin, along with higher permeation characteristics. Better formulation characteristics of in-situ hydro gels might be because of homogenous deposition and gelling of carbopol around curcumin nanoparticles.

Biography:

He was born on the 2nd of March in 1986 in Carrara (MS), Tuscany (Italy) and is currently a MD, a MSc, a PhD and a resident in Public Health. He got his MD (medical degree) on the 15th of July in 2011 with a final mark of 110/110 cum laude with a thesis on Personalized Nanomedicine ("Nanomolecular aspects of medicine, at the cutting-edge of the nanobiosciences in the field of health-care") and the joint Italo-Russian MSc (Master of Science) in nanobiotechnologies at Lomonosov Moscow State University (27th April 2012). He got his PhD in nanochemistry and nanobiotechnology at Marburg University, Germany with a final mark of “very good” and is currently a resident in Public Health at University of Genoa, Italy, 3rd year. He is author and/or co-author of several publications.

Abstract:

Ramadan fasting represents the fourth of the five pillars of the Islam creed ('aqidah). Even though patients are exempted from observing this religious duty, they may be eager to share this particular moment of the year with their family and peers, by attending the special prayers, social gatherings and other ceremonies. However, there are no guidelines or standardized protocols that can help physicians to properly address the issues and concerns of patients willing to fast in Ramadan and correctly advising them. Despite the extensive body of studies conducted on Ramadan fasting, so far only clinical parameters and analytical chemistry have been used and assessed. There is a dearth of systems biology- and omics-based studies, which investigate biological events from a global perspective, not focusing on single candidate clinical biomarkers but taking into account the entire overall perturbations, by means of high-throughput technologies. Systems biology and omics sciences could assess the metabolic effects of Ramadan fasting, confirming well-known and expected metabolic perturbations, and adding knowledge on both the short-term and long-term effects of Ramadan fasting. Systems biology and omics sciences could undoubtedly constitute a fundamental step further and a crucial advancement in the field of the relationship between religion and health. It can be anticipated that these highly advanced specialties provide a unique, unprecedented opportunity for studying the physiology and physiopathology of fasting, giving personalized counseling and advice to patients willing to fast during Ramadan.

Biography:

Tomas Etrych has completed his PhD at the age of 28 years from Institute of Macromolecular Chemistry, Academy of Sciences of the Czech Republic (IMC). He is the group-leader of Department of Biomedicinal Polymers of IMC. He has published more than 75 papers in reputed international journals, which were cited more than 1800 times and is an author of 8 patents. His research focus is based on preparation of water-soluble and micellar drug delivery systems for effective treatment of cancer.

Abstract:

Beside the development of novel low-molecular-weight anti-cancer agents, new formulations of “classic” cytostatic drugs, so called drug delivery systems (DDS), including their encapsulation into liposomes and nanoparticles or covalent binding to water-soluble polymers and micelles, appear to be a very promising strategy.Described micellar and star polymer-drug conjugates are high-molecular-weight (HMW) drug conjugates designed for enhanced passive tumor accumulation and release of drug in the acidic milieu of a tumor. Th e therapeutic effi cacy of the conjugates is based on two mechanisms of selectivity toward solid tumors: I) drug accumulation in tumors driven by enhanced permeability and retention (EPR) eff ect, which results in almost 100 times higher concentration of drug in the solid tumor than in normal tissue, II) pH-dependent release of drug from polymer-drug conjugate, which releases free drug more effi ciently at a lower pH in tumors. By the in vivo noninvasive multispectral optical imaging of fl uorescently labeled copolymers we have proven that the longer circulation times of star-like copolymers in blood led to higher accumulation in tumors. Th e same phenomenon has been observed in biodistribution studies of selected drugs. Th e tumor-to-blood and tumor-to-muscle ratio for star and micellar polymerdoxorubucin conjugates increased with time, demonstrating that the conjugates passively accumulate within a tumor mass due to the EPR eff ect. Th e anti-tumor activities of linear, micellar and star copolymers containing Dox were compared using a well-defi ned model of experimental malignant tumor, mouse EL4 T cell lymphoma, inoculated in conventional mice. Th e highest effi cacy, highest percentage of LTS, was achieved during the treatment with micellar and star conjugates. Moreover, we observed that the pH-sensitive polymer-drug conjugates have the potential to induce excellent antitumor eff ect without apparent adverse eff ects.

Biography:

Serena Mazzucchelli, PhD, fixed-term researcher at the “L. Sacco” University Hospital, Milan. She received her bachelor degree in Biological Sciences in 2004, degree in Biology in 2006 and PhD in Biological Sciences in 2009 at the Department of Biotechnology and Biosciences (University of Milan-Bicocca-Italy). From 2009 to 2012 she is post-doc at the Department of Biomedical and Clinical Sciences “L. Sacco” (University of Milan-Italy). She has a broad training in biology, biochemistry and nanobiotechnology. Her research is focused on the study of nanoparticle interaction with cells aimed at the development of nanodevices for diagnosis and therapy of breast cancer.

Abstract:

Engineered apoferritin nanoparticle (HFn) was developed to achieve a cumulative self-triggered nuclear delivery of antitumor drugs in cancer cells (CC) with subcellular precision. Th e rationale of our approach is based on exploiting the natural arsenal of defense of CC to stimulate them to recruit large amounts of HFn loaded with doxorubicin (DOX) inside their nucleus in response to a noxious stimuli, which leads to decrease of viability and cell death. Aft er demonstrating the selectivity of HFn for representative cancer cells compared to healthy fi broblasts, DOX-loaded HFn were used in CC treatment. Our results proved that loading of DOX in HFn increased the nuclear delivery of the drug, thus enhancing DOX effi cacy. DOXloaded HFn acts as a “Trojan Horse”: HFn were internalized in CC more effi ciently compared to free DOX, then promptly translocated into the nucleus following to the DNA damage caused by the partial release in the cytoplasm of encapsulated DOX. Th is self-triggered translocation allowed the drug release directly in the nuclear compartment, where it exerted its toxic action probably bypassing the action of the Glycoprotein-P. Th is approach was reliable and straightforward providing an antiproliferative eff ect with high reproducibility. Th e particular self-assembling nature of HFn nanocage makes it a versatile and tunable nanovector for a broad raange of molecules suitable both for detection and treatment of CC.

Biography:

Abstract:

Epilepsy is characterized by abnormal electrical activity within the brain, which can result in either generalized or partial seizures. In order to control seizure activity a person must take anti-epilepsy medication, normally in the form of a tablet. The goal is to deliver the drug to the brain in quantities sufficient to eliminate seizures without causing adverse effects. In 30% of the cases, sufferers of epilepsy are unable to be medicated due to the dose required to suppress seizures causing adverse side effects. In addition, other anti-epilepsy treatment such as brain surgery or vagus nerve stimulator (VNS) implantation are very expensive treatments and needs high technology and advanced equipment. Therefore there is a need to develop a delivery system for these epilepsy sufferers that is therapeutic but not toxic and also accessible and affordable for every patient all over the world. Recently there has been much interest in the use of polymeric carriers as localized delivery devices especially for the central nervous system. Bypassing the blood-brain barrier, a polymeric carrier implanted directly into the brain tissue allows the possibility of therapeutic levels of drug being confined to the region of interest, thus eliminating systemic toxicity compared to oral drug administration. Among polymers conducting polymers (CPs) have been shown to act as very effective drug reservoir with the ability to deliver drugs upon electrical stimulation. However, one limiting factor for these CP systems is their limited drug loading capacity which restricts the life time of delivery. In order to improve the drug delivery lifetime of the CP device we aimed to develop a CP drug delivery system whereby the drug is encapsulated within a reservoir and release is mitigated by opening and closing a CP “gate”. During my research designing and producing of this gate has been done. I have produced a CP gate which is a platinised PVDF membrane upon which polypyrrole with different counterions has been deposited. I have demonstrated that it is possible to open and close this gate as a function of applied electrical stimulation. Therefore, I have investigated and successfully controlled the transport of lacosamide which is an antiepilepsy drug (AED) through this gate under non-stimulated, stimulated and pulsed potential conditions. At the next stage of my research I studied the interaction of the drug molecules utilizes a hollow PVDF fibre which acts as a drug reservoir and transport gate simultaneously. The fibres are platinised and then coated with polypyrrole with different counterions. Drug release from inside of these fibres to outside has been investigated at non-stimulated, stimulated and pulsed potential states. Epilepsy is a chronic disease which unfortunately causes so many difficulties in patients’ personal life and can impose severe limitations to their life. The current antiepilepsy treatments have some severe side effects or they are very expensive treatments which is not affordable for all patients everywhere in the world. I hope my research is the beginning of a promising pathway to find a treatment for epileptic patients which can treat all of them with a reasonable price and minimum side effects, also, bring hope and happiness to their life.

Biography:

Marta Truffi is a Post-doc fellow at Centro di Microscopia Elettronica per lo sviluppo delle Nanotecnologie applicate alla medicina in University of Milano, Italy. During her studies and research activities she got interested in cell biology and differentiation, in particular how cells sense external stimuli and respond to the surrounding microenvironment. At present, her research projects aim to exploit bioengineered nanoparticles to target specifi c cellular populations in order to monitor different stages of infl ammatory bowel diseases, and further provide therapeutic benefi ts. Competences: cell culture and transfection, RNAi technology, lentivirus production, protein and RNA analysis, recombinant protein purifi cation, GST pull-down, DNA cloning and sequencing, classic and Real-Time PCR, confocal microscopy.

Abstract:

The identifi cation of new strategies aimed to optimize the detection and treatment of primary breast cancer and metastases represents a great technical and medical challenge. Target-specifi c nanodevices may allow to combine specifi c tumor recognition with the capability to act as a drug reservoir for the selective delivery of chemotherapics to tumor sites. At present, the importance of surface functionalization of nanoparticles to improve their in vivo localization at the tumor is still controversial. Here, we have designed and developed a set of multifunctional nanoprobes, modifi ed with three diff erent variants of the model antibody trastuzumab (TZ), a widely used therapeutic agent for the management of HER2-positive breast cancer. We have performed a comparative study of internalization, traffi cking, and metabolism in breast tumor cells of multifunctional nanoparticles (MNP) functionalized with either the entire TZ or alternative lower molecular weight variants of the monoclonal antibody, such as the half-chain (HC) and a single chain variable fragment (scFv). Th en, we have estimated to what extent the structure of the surface bioligand could aff ect the targeting effi ciency of the nanoconjugate in both in vitro and in vivo settings, and found that the highly stable MNP-HC is the best candidate for application in breast cancer detection. Our results provide evidence that a specifi c functionalization of nanoconstructs may aff ord long-term action in cancer cells in vivo. Furthermore, the longer period of accumulation of MNP-HC in the tumor makes this nanoparticle a promising candidate for future application in breast cancer diagnosis and treatment.

Biography:

B.Mishra is currently working as Professor and Head at Department of Pharmaceutics,IIT (BHU),Varanasi,India. He is M.Pharm . PhD ,has 30 years of teaching and research experience,and is a reputed researcher in the area of rate controlled oral drug delivery systems including nano medicines. He has produced 12 Ph,D. ,50 M Pharm, and published around 170 research/review articles, written several book chapters and has h index - 25, i10 index-58,citations more than 2600,received various awards ,delivered several talks within India and outside. He has handled several research projects as well. Currently supervising 12 students for higher degree.

Abstract:

Pastillation is a robust technology in chemical industry to convert hazardous chemical powders to solidifi ed hemispherical pellets, called Pastilles using a large equipment called “rotoformer”. In this process the dusty chemicals are heated to convert them into a melt and then this melt is dropped on a cold surface to solidify the melt into pastilles. Th ere are several pharmaceutical excipients, like waxes, lipids and PEGs, which can be liquefi ed by melting and then can be moulded into desired shape. Waxes and lipids are hydrophobic in nature and are being used to control the release of drugs in the aqueous gastric environment. On the other hand PEGs are water soluble drug carrier and can deliver the entrapped drug as soon as it comes in contact with GI fl uids. Considering above concept, we explored the possibility of utilizing pastillation technology in the design and development of oral modifi ed release multiparticulate delivery system of Doxofylline, which can be used for the better treatment of asthma and COPD. We designed a small setup of laboratory scale to prepare the pastilles. Using this technology, issues like improved patient compliance with enhanced therapeutic effi cacy of Doxofylline was addressed. Controlled release pastilles were prepared using lipids carrier for improving patient compliance. Whereas issue of enhanced therapeutic effi cacy of doxofylline, specifi cally for the management of nocturnal asthma, was addressed by designing immediate release pastilles using PEG as drug carrier, which was further enteric coated to achieve the required drug release profi le. Th e developed formulations were characterized for their physicochemical characteristics, in-vitro performance and in-vivo behaviour. Th e laboratory scale preparation of pastilles, experimental details and the fi ndings will be presented in detail.

Biography:

Abstract:

Background: Inappropriate Antibiotic (ATB) prescription threatens patients with adverse drug reactions, bacterial resistance, and subsequently elevated hospital costs. Aim of this study was to assess the incidence types of ATB prescription errors and identify their associated predictors among patients admitted to an emergency department at king Abdulaziz medical city in Riyadh. Methods: A retrospective cohort study was conducted by chart-reviewing all patients with infectious complaints over 3 months. Patient characteristics (age, gender, weight, allergy, infection type) and ATB prescription characteristics (class, dose, frequency, duration) were evaluated for appropriateness based on internationally recognized drug guidebooks. Descriptive and analytic statistics were applied. Signifi cance was set at p-value<0.05. Results: Total of 5,752 patients had equal distribution by gender(males 49%,females 51%) and age groups (adults 61%,pediatrics 39%), of which 55% complained respiratory tract infections(RTIs), 25% urine tract infections(UTIs), 11% otitis media (OM). Broad spectrum ATBs were prescribed for 77% of the cases. Prior prescription in pediatrics, 82% had weight taken. Incidence of ATB prescription with at least one type of error was 58% in pediatrics and 39% in adults. Errors were in selection of ATB class (2%), Dose (21%), Frequency (6%), and Duration(25%). Dose/duration errors were signifi cantly predominant among pediatrics (p=0.0001/p<0.0001 respectively). Selection error was higher among adults (p=0.002). Age stratifi cation and binary logistic regression were applied. Signifi cant predictors of errors in both age groups were associated with penicillin prescriptions (adult: p<0.001 ,adj.RR=3.09), (pediatric :p<0.001,adj.RR=4.10) compared to cephalosporin & with RTIs (adults: p<0.001,adj. RR=2.82), (pediatrics: p=0.039,adj.RR=1.37) compared to UTIs & with obtaining weight for pediatrics prior prescription (p<0.001,adj.RR=1.83) compared to those who didn’t. Conclusion: Incidence of ATB prescription errors in this ED was alerting and high compared to similar studies. Setting clear and accessible guidelines for antibiotic prescriptions especially for narrow spectrums and UTI infections is recommended. Inappropriate antibiotic prescription is the responsibility of institution, and community as well, to reduce the emerging resistant bacteria, and cost especially.

Biography:

Rachad Alnamer has completed his PhD at the age of 36 years from Faculty of Medicine and Pharmacy, Mohammed V Souissi University, Rabat, Morocco. He is the president of the Pharmacy section in University of Thamar, Yemen. He has published more than 22 papers in reputed journals and has been serving as an editorial board member of repute (more than 30 reputed journals).

Abstract:

In this study, the in vitro cytotoxicity and antioxidant properties of the ethanolic and alkaloidic extract of Delphinium staphisagria seeds were assessed. Th e antioxidant activity of the plant extracts and the standard was assessed on the basis of the radical scavenging eff ect of the stable 1, 1-diphenyl-2-picrylhydrazyl (DPPH)-free radical activity. Th e in vitro cytotoxicity was carried out by using the 3-(4,5- dimethylthiazol- 2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay, against two animals cancer cell lines; Vero cell line, initiated from the kidney of a normal, adult African green Monkey and Neuro-2a (N2a) from a spontaneous tumor of a strain A albino mouse. Th e DPPH scavenging activity of both extracts was concentrationdependent (increasing from 15.62 μg/ml to 500 μg/ml), exhibited considerably (P<0.05) DPPH radical-scavenging activity and was able to inhibit the formation of DPPH radicals with a percentage inhibition of 62.19 and 94 % respectively at the highest concentration. Th e results showed that the alkaloidic extract (1000-31.25 μg/ml) of Delphinium Staphisagria possesses signifi cant IC50 compared to the drug positive control on all cancer cell lines used.Th e lower IC50 represent the highest potency of a compound to inhibit the growth of cells and cause toxicity and death of cells. Th e result obtained in this work demonstrated a high activity at low alkaloids extracts doses (500μg/ml).In conclusion, the results of the present study suggest that Delphinium staphisagria seeds plant have various secondary metabolites and has good quantity of alkaloidic compounds (diterpenoid alkaloids). Plant has potent free radical scavenging activity. Detailed studies on chemical composition, isolation of active constituents and pharmacological evaluation are essential to characterize them as biological antioxidants. Th e present fi ndings of this study support the view that Delphinium staphisagria seeds are a promising source of potential antioxidant which can be used in treatment of various ailments.

Biography:

Abstract:

Background/ Aim: Sirolimus (SR) is highly protein binding drug (92%) and lipophilic (log P=4.917) in nature. It has half life of 57-63 hrs and oral bioavailability is 20% even less when aft er eating food rich in fat. In our objective of the study, SR is chemically conjugated with biodegradable polymers like Methoxy-polyethylene glycolic acid (mPEG COOH) and Poly(Lacticco glycolic acid)(PLGA) .It was ensured that there is a structurally correlation among the chemical structures of SR, mPEG COOH-SR conjugate, PLGA-SR conjugate, PLGA and m-PEG COOH polymers. Methods/Materials: Th e cytotoxicity assay of both conjugates was carried out on specifi c A-549 lung cancer and HT-29 colon cancer cell lines using vincristine sulfate, tamoxifen and cisplatin as controls separately. Results: All results were showing the positive eff ects of PLGA-SR and cisplatin with IC50 values of 2.88 μg/ml and 9 μg/ml indicatively more active than cisplatin in vitro. Whereas mPEG-SR conjugate was similar activity of cisplatin with IC50 value of 8.88 μg/ml on A-549 lung cancer cell line. Both conjugates were not shown any cytotoxicity activity on 3T3 fi broblast normal cell lines. On the other hand, PLGA-SR conjugate was nine times more active than vincristine sulfate with IC50 value of 7 μg/ ml, where as MPEG-SR conjugate is more active than other controls and SR alone on HT-29 colon cancer cell line. Th ese results are indicated that both conjugates with potent cytotoxicity activity against specifi c lung cancer and colon cancer types than SR alone. Conclusion: Polymeric conjugation is a useful approach in a novel drug delivery system. Th ese conjugates are basic precursors to formulate into novel drug delivery systems especially in as nanocarriers for better release with surface modifi cation to enter the tumor cells with signifi cant increase in the bioavailability.

Biography:

Abstract:

Benzopyrano-pyrimidine derivatives (3a-c and 4) were prepared viacyclocondensation of 3-ethoxycarbonyl coumarin derivatives (2a-c) with guanidine hydrochloride and thiourea under refl ux. Acetylation of (3b, c) with acetic anhydride provided N-acetyl derivatives (5a, b) - imidazolo-[2,1-a]-benzopyrano [4, 3-d]-pyrimidin-1, 6-dione (6) was obtained by treatment of 2-amino-benzopyrano[4,3-d]-pyrimidine with ethylchloroacetate. Structures of these compounds were established on basis of IR, 1H-NMR and MS data. Some of the prepared compounds were evaluated for antimicrobial and antitumor activties.

Biography:

Julia Rohrer is doing her PhD at the University of Innbruck, Austria. She received her degree in Pharmacy at University of Munich, Germany in 2011.

Abstract:

Aim: Th e aim of the study was the development of a novel self micro emulsifying drug delivery system (SMEDDS) to overcome the mucus barrier in the small intestine. Methods: Two novel conjugates thiobutylamidine-dodecylamine (TBA-D) and thioglycolic- acid-octylamine (TGA-O) were synthesized and incorporated into SMEDDS in a percentage of 3% (m/m). N-acetyl-cysteine NAC served as control. SMEDDS were screened for stability, cytotoxicity, size, zeta potential, diff usion coeffi cient, homogeneity of micelles movement and eff ective diff usivities and mucolytic activity. Results: TBA-D was synthesized using dodecylamine and iminothiolane as thiol precursor. TGA-O was obtained via cross linking of octylamine with SATA ((2, 5-dioxopyrrolidin-1-yl) 2-acetylsulfanylacetate). NMR spectroscopical measurements gave proof of successful thiolation. Micelle size was recorded around 50nm; the zeta potential was near zero mV. Th e diff usion coeffi cient in mucus showed an 87-fold increase for SMEDDS containing TBA-D compare to NAC SMEDDS which showed an increase of 24-times. TBA-D could decrease the diff erence between slowest and fastest percentile of up to 52-times. Eff ective diff usivity for the majority of the micelles of TBA-D SMEDDS is diff usive through mucus compared to the control for which 81% were not. Rheological studies of thiol compounds proved a decrease in mucus viscosity of up to 43%. Conclusion: Th iol-conjugates were identifi ed to strikingly improve mucus permeation of SMEDDS due to their mucolytic activity. Th is can be regarded as unmet need for small intestinal targeting. Drug delivery systems, which are able to permeate the mucus might thus be a superior drug delivery system for poorly water soluble drugs.

Biography:

Alexandra Partenhauser is writing her PhD thesis on polymeric drug delivery systems under the supervision of Prof. Bernkop-Schnurch in Innsbruck, Austria and has already published one paper in a well reputed journal within her fi rst year. She previously fi nished both her Master of Pharmaceutical Sciences and studies of Pharmacy in Munich, Germany, where she was part of a project on an ocular sustained delivery system in the research group of Prof. Winter for her Master thesis.

Abstract:

Aim: Th e purpose of this study was the evaluation of thiolated silicone oil as novel skin protectant with a prolonged residence time, enhanced barrier function and reinforced occlusivity. Methods: Two silicone thiomers were synthesized with mercaptopropionic acid (MPA) and thioglycolic acid (TGA) as thiol ligands. Adhesion, protection against artifi cial urine as well as water vapour permeability with both a Payne cup setup and transepidermal water loss (TEWL) measurements on porcine skin were performed. Results: Silicone conjugates showed pronounced substantivity on skin with 39.2 ± 6.7 % and 22.1±6.3 % remaining silicone aft er 8 h for silicone-MPA and silicone-TGA, respectively, whereas unmodifi ed silicone oil and dimethicone were no longer detectable. Especially silicone- MPA strikingly shielded skin against artifi cial urine penetration for up to 6 h and showed a reduced TEWL by two third in comparison to control. Conclusion: Th iolation of silicone oils leads to enhanced skin adhesiveness due to disulfi de crosslinking, which is a major advantage compared to commonly used silicones, such as dimethicone. Depending on the thiol ligand, various degrees of occlusivity can be achieved. Th iolated silicone oils thus provide a protective layer and improve skin moisturization. Pharmaceutical targets might be hypertrophic scars and keloids, neurodermatitis, psoriasis as well as atopic, allergic or irritant contact dermatitis.

Biography:

Blanka Suto is currently a PhD student in the Department of Pharmaceutical Technology at the Doctorate School Programme of Pharmaceutical Sciences, Faculty of Pharmacy, University of Szeged. Her research work focuses on the preformulation, production and characterization of solid lipid nanoparticles and nanostructured lipid carriers intended for topical use.

Abstract:

Ibuprofen is a potent NSAID oft en used treating acute- and chronic arthritic conditions or acute pain. Its low water-solubility and low bioavailability are great challenge in the development of dermal delivery. One approach for overcoming this problem is the use of lipid nanoparticles. Lipid nanoparticles are intensively studied drug delivery systems derived from o/w emulsions. Th e oil phase is replaced by a lipid (or mixture of lipids) which is solid at both room and body temperatures. Th ere are two generations of lipid nanoparticles: Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC). Lipid matrix of SLN is produced only from solid lipid(s), while matrix of the NLC consists of a blend of both solid- and liquid lipid(s). Th ese particles are stabilized by surfactants in an aqueous solution. Advantages of NLC systems compared to SLN are higher drug loading capacity and steady drug entrapment during storage. Th e dermal use of NLC systems off er a number of advantages such as physical stability of the applied topical formulations, enhancement of chemical stability of the incorporated drugs, improved skin bioavailability and skin targeting of actives, fi lm formation on the skin accompanied with controlled occlusion, skin hydration in vivo. UV refl ecting properties and the opportunity of modulate drug release into the skin has been also reported. Th e aim of this study was the development and characterization of ibuprofen loaded NLC for dermal drug delivery by means of particle size measurements, zeta potential, drug permeation studies and Raman spectroscopy.

Biography:

Gabriella Horvat is a PhD student at the University of Szeged, in the Department of Pharmaceutical Technology. Her research work is on the subject of mucoadhesive polymers, especially thiolated polymers and hyaluronic acid derivatives. The target of these mucoadhesive polymers is the eye in order to increase the low bioavailability of the ophthalmic preparations. During her PhD studies she has spent four months in Italy at the University of Pavia, in the Department of Drug Sciences to gain experience on the subject of mucoadhesion. Her works were presented on domestic and international conferences

Abstract:

With the aging of the population, the need for treatments for ocular diseases and disorders has become more important than ever. If we aim to maintain the quality of life for this aging population, the preservation of vision is critical. Since topical ocular delivery treatments are considered to be the safest, least invasive, and most self-administrable, their development is highly sought. Unfortunately, the application of formulations available on the market have many disadvantages such as the need for frequent instillation of eye drops, which is accompanied by discomfort and a decrease in patient compliance, especially in long-term therapy. One way to overcome these drawbacks is to formulate a drug delivery system with mucoadhesive properties leading to the increase of residence time of the drug on the ocular surface, drug uptake, diff usion and transport, while the concentration, required volume and usage frequency can be decreased. Th e aim of our work was to determine the properties of thiolated poly(aspartic acid) (Th ioPASP) polymers as potential in situ gelling, mucoadhesive ophthalmic drug delivery system. Mucoadhesion measurements were performed in vitro (rheology, tensile test) and ex vivo (tensile test, “wash away” test). Th e release of sodium diclofenac, a frequently used non-steroidal antiinfl ammatory drug with low bioavailability, from the gels was also determined. According to all results Th ioPASP polymers can serve as potential ocular mucoadhesive drug delivery systems with an appropriate drug release profi le whereby the administration frequency can be decreased and the patient compliance might be increased. Th is work was supported by Campus Hungary fellowship.

Biography:

Abstract:

Purpose: To study the in vitro release behaviour of combination of metronidazole (MTZ) and doxycycline (DOX), from polycaprolactone (PCL) matrices, intended for production of vaginal rings for the treatment of pelvic infl ammatory disease (PID). Methods: Combination and individual Metronidazole and doxycycline was incorporated in PCL matrices at varying loading doses prepared by rapidly cooling suspensions of the drug powder in acetone solutions of PCL. Daily and cumulative release amounts of the drugs were determined in SVF by HPLC assay. Th e in vitro antibacterial activity of metronidazole on Gardnerella vaginalis and Doxycycline on Neisseria gonorrhoea was tested using disc diff usion method. Cell toxicity and irritation of the released material will be tested on vaginal cell line. Results: Aft er 14 days immersion in SVF, the PCL matrices released from 20 to 60% of DOX and 15-40% of MTZ and when they were studied in combination 15-60% DOX and 30-60%MTZ has been released over 7 days period. Aft er 7 days the amount of metronidazole released is less than the minimum inhibitory concentration so these matrices are useful only for 7 day period. 80-90% of activity has been retained for both released MTZ and DOX compared to the standard drug. Conclusion: Th ese fi ndings indicate that the PCL could be a potential polymer for the intravaginal delivery of combination of antibacterial for the treatment of PID.

Biography:

Abstract:

Due to the lower risk of systemic side eff ects, topical treatment of skin disease appears favorable, yet the stratum corneum counteracts the penetration of xenobiotics into viable skin. Fatty acids have been widely used as adjuvant, vehicles in drug delivery viz. penetration enhancers in topical delivery and in polymeric micelles to provide sustained release. However, the present investigation aims at exploring the potential of fatty acid vesicles for the topical delivery of Disease modifying Anti-rheumatic drugs (DMRD’S). Vesicles were prepared by fi lm hydration method using oleic acid as a fatty acid principal component. Developed vesicles were characterized for size, size distribution, shape, In vitro release, pH dependent and storage stability, skin and ex-vivo skin permeation. Optical microscopy and TEM studies confi rmed vesicular dispersion of fatty acid. Ex-vivo skin permeation and Confocal microscopic (CLSM) studies suggested that oleic acid vesicles penetrate the stratum corneum and retain the drug accumulated in the epidermal part of the skin. On the basis of sustained release behavior and skin retention it can be inferred that oleic acid vesicles can serve as a potential carrier for the topical localized delivery of bioactives.

Biography:

Kanav Midha, a post graduate fellow, Chitkara University, India. He is currently working on research project entitled Utility of modifi ed locust bean gum for dissolution improvement of poorly soluble drug. Before joining as post graduate fellow, he had completed Bachelor’s in Pharmacy from Swami Vivekanand Group of Institutes and worked with Medtronic India for 7 months. He is a life time member of Indian Pharmacy Graduates Association and has attended various National and International conferences in India.

Abstract:

The present research was aimed at the enhancement of the dissolution rate of glimepiride by the solid dispersion technique using modifi ed locust bean gum. Th e locust bean gum was subjected to heat for modifi cation. Modifi ed solvent evaporation technique was used to prepare solid dispersions (in various drug: polymer ratios). Other mixtures were also prepared by physical mixing, co-grinding, and the kneading method. Various solid dispersions and other mixtures were evaluated for equilibrium solubility studies, content uniformity, FTIR, DSC, XRD, in vitro drug release, and in vivo pharmacodynamic studies. Maximum equilibrium solubility was observed in the solid dispersions SD3 (in a drug: polymer ratio of 1:6) and cogrinding mixture also showed equivalent solubility. Maximum dissolution rate was observed in the solid dispersion batch SD3 (i.e. 48% within 15 min) with maximum drug release aft er 2 h (89%). Th e co-grinding mixture also exhibited a signifi cant enhancement in the dissolution characteristics (45% in 15 min and 85% aft er 2h) among the other mixtures. FTIR studies indicated the absence of drug-polymer interaction in the solid dispersions, which was further supported by XRD studies. Minor shift s in the endothermic peaks of the DSC thermograms of SD3 and CGM indicated slight changes in drug crystallinity. Topological changes were seen in SEM images of SD3 and CGM. In vivo pharmacodynamic studies indicated an improved effi cacy of the optimized batch SD3 as compared to the pure drug (p≤0.05). Reduction in particle size, decreased crystallinity of drug with less viscosity and wetting ability of modifi ed locust bean lead to enhanced dissolution characteristics. Th e cogrinding mixture can be a good alternative to solid dispersions.

Biography:

SAJEEV KUMAR.B (PhD) is a research scholar at JNTUH, Hyderabad, India. Presently he is working as Associate Professor in Karavali College of pharmacy, Karnataka. He has 13 years of teaching and research experience and has guided 10 post graduates and 36 under graduates. He has served as senior lecture at AIMST University, Malaysia for a period of 5 years. He was awarded with the best research paper on ‘Nanocrystals’ at Ist International Conference on Nutraceutical and Cosmetics Sciences (ICNaCs - 2012) held at Kuala Lumpur Malaysia. He has published more than 20 papers in peer reviewed journals and has been serving as an editorial board member of repute.

Abstract:

Nanoparticulates (NPs) are developed with an aim to improve the solubility, targetability and bioavailability of a drug. Lipid Complexed Nanocrystals (LNCs) are novel and unique nanoparticulates off ering high solubility and stability both in vitro and in vivo, hence making it more sustain to body fl uids (electrolytes). In vitro instability (particle aggregation) of NPs may decrease its functional behavior in vivo leading to decreased bioavailability. Development of functional NCs requires modifi cation of its surface properties in sequence to make them clinically more acceptable. Th e study aim to develop Glimepiride NCs using PEG 20000 by nanonization (precipitation) and stabilize them (both in vitro and in vivo) by complexation using Phospholipon 90 G (P 90G). Particle and solid state characterization studies were performed on NCs before and aft er complexation using photon correlation spectroscopy (PCS) and X-ray diff raction spectrometry (PXRD), differential scanning calorimetry (DSC), scanning electron spectroscopy (SEM) and fourier transform infrared spectroscopy (FTIR). In vivo drug targeting effi cacy of LNCs was studied on pancreas of Male Wistar rats using HPLC. Th e particle and solid state characterization results show improved stability (decreased aggregation) with no change in drug properties aft er complexation. In vivo results on optimized LNCs show similar drug concentration in pancreas of rat as that of pure drug. AUC was signifi cantly higher aft er 1 h signifying better in vivo stability. It can be concluded that in vitro and in vivo stability of NCs could be achieved by a complexation using P90 G. Th e possible outcome of these studies could result in development and delivery of stable and safe nanoproducts in the treatment of diabetes.

Biography:

Maha Aboul Ela, graduate of Faculty of Pharmacy, University of Alexandria, Egypt. Ph D in Pharmaceutical Sciences (Pharmacognosy) 1991, University of Alexandria-Egypt and Technical University of Berlin-Germany. She had done her Postdoctoral fellowship, from School of Pharmacy, University of London, UK. She is Member of the American Society of Pharmacognosy. She is also Member of the editorial board of many international scientifi c journals. Currently, she is head of department of Pharmaceutical Sciences, Faculty of Pharmacy, Beirut Arab University, Lebanon.She is Expert in QA in Higher Education. Research interest: Phytochemistry, Phytotherapy, discovering new drugs from natural sources and participation in drug development through applying different pharmaceutical approaches, more than 55 publications in the fi eld of phytochemistry, medicinal plants and phytotherapy.

Abstract:

The Middle East region is a major source of phytotherapeutic natural products. Different pharmacological studies on the Middle East medicinal plants revealed their signifi cant importance as new sources of drugs. Focusing on endocrinal and neurological diseases, a number of Middle East plants had shown signifi cant potentials towards these diseases. Salvia libanotica fruticosa, Centaurea horrida; Hordeum spontaneum and Rheum ribes are herbal plants indigenous to ME region and had shown notable eff ects on Diabetes mellitus and one of its related complication; the painful diabetic neuropathy. Diabetic neuropathy is the leading cause of neuropathy in the world today. Diabetic neuropathy has a few approved therapies for the management of pain with limited effi cacy and side eff ects. With the aim to explore and develop new phytotherapeutic agents, we investigated the antidiabetic and antihyperalgesic properties of some Middle East natural products in alloxaninduced diabetic mice. Th e results of our experiments indicated that, these plants exhibited a remarkable effect against diabetic neuropathy. More experiments should be done to complete these plants’ profi le before their dispensing in suitable dosage forms to facilitate their delivery to the targeted sites.

Biography:

Hassane Sadou Yaye completed his Pharma D and, he is head of the laboratory of quality control of pharmaceuticals in the department of Pharmacy (Pitie- Salpêtriere hospital - Paris); and PhD student (University Paris Sud). His research focuses on APIs intrinsic stability studies which include the structure elucidation and the main routes of their degradation.

Abstract:

Ticagrelor is a direct-acting and reversible P2Y12-adenosine diphosphate (ADP) receptor blocker used as antiplatelet drug. Th e drug was subjected to force degradation studies under several stress media. Th e degradation products generated have been detected and identifi ed by high-pressure liquid chromatography multistage mass spectrometry (LC-MSn) along with high-resolution mass spectrometry. C18 XTerra MS column combined with a linear gradient mobile phase composed of a mixture of 10 mM acetate ammonium/ acetonitrile was shown suitable for drug and impurity determinations and validated as a stability indicating method. Structural elucidation of the degradation products relied on MSn studies and accurate mass measurements giving access to elemental compositions. Up to nine degradation products resulting from oxidation/ autooxidation, S-dealkylation and N-dealkylation have been identifi ed, covering a range of possible degradation pathways for derivatives with such functional groups. Kinetics was also studied in order to assess the molecule’s shelf-life and to identify the most important degradation factors. Eventually, an in silico toxicological study was undertaken starting from the structure of the degradation products in order to know any potential risk resulting from drug degradation.

Biography:

Abstract:

The performance of the novel chitin metal silicate (CMS) co-precipitates as a single multifunctional excipient in tablet formulation using direct compression and wet granulation methods is evaluated. Th e neutral, acidic, and basic drugs Spironolactone (SPL), ibuprofen (IBU) and metronidazole (MET), respectively, were used as model drugs. Commercial Aldactone®, Fleximex® and Dumazole® tablets containing SPL, IBU and MET, respectively, and tablets made using Avicel® 200, were used in the study for comparison purposes. Tablets of acceptable crushing strength (>40 N) were obtained using CMS. Th e friability values for all tablets were well below the maximum 1% USP tolerance limit. CMS produced superdisintegrating tablets (disintegration time < 1 min) with the three model drugs. Regarding the dissolution rate, the sequence was as follow: CMS > Fleximex® > Avicel® 200, CMS > Avicel® 200 > Dumazole® and Aldactone® > Avicel® 200 > CMS for IBU, MET and SPL, respectively. Compressional properties of formulations were analyzed using density measurements and the compression Kawakita equation as assessment parameters. On the basis of DSC results, CMS co precipitates were found to be compatible with the tested drugs. Conclusively, the CMS co-precipitates have the potential to be used as fi ller, binder, and superdisintegrant, all-in-one, in the design of tablets by the direct compression as well as wet granulation methods.

Biography:

Hijazi Abu Ali is an associate Prof. in the field of medicinal and bioinorganic chemistry. He is the chairperson of Chemistry Department at Birzeit University, Palestine. He has published more than 30 publications (papers, reviews, books) in reputed journals and agencies. In addition he has been serving as a reviewer for several journals.

Abstract:

Starting from the precursor [zinc carboxylate complex], where (carboxylate = valproate, naproxenate, ibuprofenate, indomethacinate, diclofenate and sulindaco) and nitrogen based ligands, different Zinc(II) complexes with the general formula [Znm(carboxylate)n(L)x] where; (L = 2,9-dimethyl-1,10-phenanthroline, quinoline, 2-aminopyridine, 2-amino-6-picoline, 2-aminomethyl pyridine, 1,10-phenanthroline, imidazole, 2,2’-bipyridine and 4,4’-bipyridine) were synthesized and characterized using IR, 1H NMR, 13C{1H} NMR and UV-Vis spectrometry. The crystal structures of some complexes were determined using single-crystal X-ray diffraction. The complexes were also evaluated for their anti-bacterial activity using in-vitro agar diffusion method against three Gram-positive (Micrococcus luteus, Staphylococcus aureus, and Bacillus subtilis) and three Gram-negative (Escherichia coli, Klebsiella pneumoniae, and Proteus mirabilis) species. Most complexes showed considerable activity against all tested microorganisms and the effect of complexation on the anti-bacterial activity of the parent ligands was also investigated. The anti-bacterial activity of some complexes against Gram-negative and Gram-positive bacteria was enhanced upon complexation, other complexes showed weak inhibition activity against the tested species. On the other hand some complexes didn’t show any activity at all. Two methods were used for testing the inhibition of ferriprotoporphyrinIX bio-mineralization: a semi-quantitative micro-assay and a previously self-developed quantitative in-vitro method. Both were used to study the efficiency of these complexes in inhibiting the formation of the Malaria pigment which considered being the target of many known anti-malarial drugs such as Chloroquine and Amodiaquine. Results showed that the efficiency of some complexes preventing the formation of β-Hematin was 80 % or higher. The efficiency of Amodiaquine as a standard drug was reported to give 91 %.

Biography:

Dr. Hsing-Pang Hsieh has completed his PhD in 1993 from SUNY at Stony Brook, USA and postdoctoral studies from Boston College, USA and Academia Sinica, Taiwan. He is Investigator of Institute of Biotechnology and Pharmaceutical Research, National Health Research, Institutes. He has published more than 100 SCI papers and obtained 43 patents granted and invented anticancer drug, DBPR104, which is currently undergoing clinical trial in Taiwan.

Abstract:

Aurora kinases A, B, and C, members of sereine/threonine kinase, are key mitotic regulators involved in maintaining the genomic integrity of daughter cells. Because over-expression of Aurora A and Aurora B is frequently associated with tumorigenesis, these molecules have been targeted for cancer therapy. Based on the structural analysis of the known Aurora kinase inhibitors and pharmacophore screening from in-house HTS compound library, we developed BPR1K0871 as the 4th generation of lead compound. BPR1K0871 was identified as a novel multiple target kinase inhibitor that possessed an impressive inhibition activity in Aurora-A kinase (IC50 = 22 nM), FLT-3 kinase (IC50 = 19 nM) and other 17 oncogenic related enzymatic assays in nano molar range. It not only showed potent cell growth inhibitory activity against a panel of various cancer cell lines, but also exhibited highly potent in-vivo efficacy in MOLM-13, MV4;11, MIA-Paca2, AsPC-1 and Hep3B subcutaneously xenografted nude mice models by iv. administration. To further improve the pharmacokinetic properties of BPR1K0871 by utilizing “drug-Like” properties optimization, prodrug, and oral formulation approaches, we identified several potent compounds that display promising oral bioavailability. In particular, BPR1K1201 not only possesses remarkable in vitro potency but also significantly improved pharmacokinetic profiles to achieve high oral bioavailability (~46%). This breakthrough finding has fueled our interest and focuses on identifying orally active anticancer drug.

Biography:

Abstract:

Solid and semi-solid dosage forms are the most widely marketed and administered drugs nowadays. Almost 70% of the administered drugs are in solid states. It is preferred by the pharmaceutical companies due to its high safety, low cost and marketing issues. Pre-formulation is a stage of development during which the physicochemical properties of drug substance are characterized. Before the formulation of a drug substance into a dosage form, it is essential that to be chemically and physically characterized. Pre- formulation begins with calculation/prediction ‘in silico’ of many of the important physicochemical characteristics of the API. Literature search of similar type of compounds is the second step of pre-formulation process. Pre-formulation infl uences on selection of the drug candidate itself, selection of formulation components, API & drug product manufacturing processes, determination of the most appropriate container closure system, development of analytical methods, assignment of API retest periods, the synthetic route of the API and toxicological strategy. Th e most important function of pre-formulation stage is solid state characterization which determines the next step in the formulation work of the studied API. Physical properties of the studied API infl uence on its physical and chemical stability. It infl uences on the rout of administration, delivery system and the drug activity. Moreover, Chemical stability of the drug is aff ected by the physical properties. Crystal morphology, polymorphism, amorphous forms and hygroscopicity are usually studied. In addition, solubility, salt form, melting point, dissolution of the API are also studied. Certain properties are studied in pre-formulation stage of the solid dosage forms. Th ese properties relate mainly to the ability of the powder to fl ow in the compressing machine and subsequently its compressibility. Th ey infl uence on the dissolution rate of the API, stability, bioavlaibility, degradation rate and purity. Th e studied properties include particle size, its distribution, its surface area and porosity. It includes also true density, fl owability, API color, electrostaticity, caking and polymorphism.