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

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.