8^th International Conference and Exhibition on Pharmaceutics & Novel Drug Delivery Systems March 07-09, 2016 Madrid, Spain

David Veale, R&D Associate at RB. BSc (Hons) in Chemistry from the University of Newcastle. David has worked for several years within RB across a range of R&D healthcare departments, and currently works in the Respiratory R&D team. David has experience in formulation and analysis of prescription, pharmacy and GSL medicines within the RB portfolio. His current role is innovation focussed and spans brands including Strepsils, Mucinex and Lemsip. Prior to RB, David had begun his industrial career in QC analysis of the nutritional content of food products.

Sore throat sprays provide targeted relief by delivering the active ingredient directly to the site of pain. Although there are several throat sprays available, they vary with respect to the spray pattern, thus affecting delivery of the active ingredient to the throat. The characteristics and performance of flurbiprofen 8.75 mg sore throat spray were compared with 12 competitor sprays. Parameters assessed include spray pattern, spray angle, droplet size, distribution, uniformity of dosage units and number of doses per bottle. Studies were conducted by an independent agency and tests were automated. The analysis showed that flurbiprofen 8.75 mg sore throat spray had the second tightest spray angle (51°), producing a more targeted dose than most competitors. Droplet size distribution studies showed flurbiprofen 8.75 mg sore throat spray had the second smallest droplet size and was therefore one of the more mist-like sprays, ensuring gentle delivery of the dose to the throat with negligible risk of aspiration into the lungs. Analysis of the spray pattern showed that the spray volume delivered, and diameter of the area covered, was uniform and consistent throughout the whole container life. Flurbiprofen 8.75 mg sore throat spray also consistently delivered an accurate dose each time. These results show that flurbiprofen 8.75 mg sore throat spray performed well overall, providing a consistent, gentle and accurate dose of medication throughout the whole container life.

Tina Kauss (PharmD at University of Bordeaux and Master 2 of Pharmaceutical technology and Biopharmacy at University Paris 11) completed her PhD in 2007 at Bordeaux’s University, followed by 3 years of postdoctoral studies in pharmaceutical development (pharmaceutical technology, biopharmacy and analytical chemistry). Since 2011 she is assistant professor of Pharmaceutical technology and Biopharmacy at the University of Bordeaux. She has published 16 papers in reputed journals of pharmaceutical development.

SEDDS (self emulsifying drug delivery system) are commonly used for absorption enhancement of poorly soluble active pharmaceutical ingredients (APIs). However, when generating in situ a nanoemulsion, beside common absorption via drug passive diffusion, additional mechanisms like lymphatic absorption of nanodrops can occur. The aim of our work was to evaluate whether a SEDDS formulation can improve the bioavailability of highly soluble, but weakly permeable drug (class III of Biopharmaceutical classification system, BCS). An additional challenge was to adapt the formulation to rectal route, where the quantity of physiological liquid for emulsion reconstitution is limited. Ceftriaxone was used as a model drug of BCS III API. Reportedly, ceftriaxone rectal absorption is very low, about 3% if not accompagnied by an absorption enhancer. From previous studies (Roche’s personal communication), sodium chenodeoxycholate was chosen as optimal absorption enhancer for all tested formulaitons. To define the formulation, a screening of oily vehicles, surfactants and co-surfactants was performed using ternary diagrams. The formulation was further optimized by 23 full factorial design. The impact of formulation on dissolution rate, size of droplets after reconstitution, time necessary for reconstitution were considered. In vivo bioavailability of the selected SEDDS formulation was further assessed in rabbits and compared with oily suspension and IV route.

Dolores Torres is Associate Professor of Biopharmaceutics and Pharmaceutical Technology at the University of Santiago de Compostela (USC) since 1990. She joined the Nanobiopharmaceuticals Group since its creation at the USC. She is experienced in the design and development of nanoparticulate drug delivery carriers for oral peptide delivery and cancer targeting. She has participated in more than 30 research projects with public institutions, and also 8 contracts with pharmaceutical companies (inventor of 4 patents). She is author of more than 50 scientific articles with more than 1,300 cites (H factor 19) and has supervised 10 PhD students.

Our lab has shown that polymer nanocapsules are an attractive vehicle for the delviery of anticancer drugs. Here we describe a new prototype; hyaluronic acid (HA) nanocapsules intended to delivery drugs intracellularly. HA-NCs were formulated by a self-emulsifying method, which makes them suitable for the manipulation and formulation of very sensitive molecules. These NCs were designed to efficiently encapsulate an hydrophobic anticancer drug in the oily core, and for the association of proteins to the polymeric shell. In this work, we present the results obtained using nile red, as small molecular weight hydrophobic drug model, and a labelled large protein model. After the optimization of the different prototypes, empty HA-NCs showed a particle size around 130 nm and negative zeta potential. For both types of model drugs, high encapsulation efficiency values were obtained. In both cases, empty and loaded HA-NCs maintained their stability after the incubation in PBS, RPMI culture medium and human blood plasma. Confocal microscopy images showed the ability of HA-NCs to transport the protein and the fluorophore to the intracellular compartment. The delivery of proteins for specific intracellular targeting is an ambitious approach where polymeric NCs appear as promising carriers for accurate delivery. The proposed system offers the additional advantage of co-delivering both drugs to reach their intracellular targets.

D Teijeiro-Osorio holds a PhD in Pharmaceutical Technology and has over 14 years of experience, in both academic and private sectors, in research and development of nanotechnology-based drug/biopharmaceutical formulations and medical devices aimed to address unmet clinical needs. In 2013, she joined Prof. Alonso´s group (USC) as Scientific Project Manager, focusing her activities on management of industry-collaborative and translational research projects.

Chitosan-based nanoparticles are versatile, biocompatible and biodegradable systems with low toxicity profiles, which make them very interesting for a huge range of applications. Additionally, they can can be readily modified and obtained by ionic gelation; an easy, mild and scalable method. All these properties have led to a worldwide study of these nanosystems, being mucosal peptide-delivery one of the most explored and promising applications. Nevertheless, the oral administration of chitosan nanoparticles comes across a really adverse physiological environment, which causes an immediate peptide release and prevents the effective interaction of both the peptide and nanocarrier with the absorptive epithelium. In order to improve the stability of these nanoparticles and obtain a controlled release of the active molecule, this work was focused on the incorporation of chitosan nanoparticles into a protective matrix. The approach followed was based on the design of an inert matrix of hydroxypropylmethylcellulose in which chitosan nanoparticles were embedded. For this purpose, nanoparticles were freeze-dried in presence of different molecular weights and concentrations of this neutral polymer was further characterized. Peptide release from the nanoparticles-containing matrixes was efficiently controlled in simulated biorelevant media, being the molecular weight and concentration of the polymer the key modulating factors.

N Storozhylova is a Erasmus Mundus NanoFar PhD student at University of Nantes and University of Santiago de Compostela, 2013-2016.

Galectin-3 (Gal-3) is a human protein able to bind sugar β-galactoside motifs and devoid of enzymatic activity. Extracellular Gal-3 was found to control and participate in immune and inflammatory responses, favouring macrophage pro-inflammatory cytokine secretion and involved in cartilage remodeling and bone erosion. It is believed that extracellular Gal-3 inhibition is a potential strategy for rheumatoid arthritis (RA) treatment and it can present a platform for the development of a new therapy approach. Previously, we reported the synthesis of Gal-3 inhibitors as anti-RA drugs. Here, we describe the formulation of this potential drug in a delivery system that is adequate for intra-articular injection. The delivery system consist of hyaluronic acid (HA) constructs containing Gal-3 inhibitor, dispersed in a modified HA hydrogel. The constructs’ parameters allow them to stay invisible for macrophages and target specifically extracellular Gal-3. Hydrogels form in situ after the injection of components solution and have well defined and controlled gellation time of 2 min. Their porous structure is sufficient for maintaining the Gal-3 inhibitor constructs. Maximal loading of them to in situ hydrogels is 30% with the gellation time of 20 min.

Ana Isabel Fraguas Sánchez has completed her Pharmacy degree in 2012 at Complutense University of Madrid. In 2013 she finished her Master’s degree in Pharmacy and Pharmaceutical Technology, with an experimental study entitled “Development of Cannabidiol Microparticles”. Currently, she is a PhD student at Complutense University. In 2014, she got an research Fellowship from Education Ministry of Spain and she has published several papers related with cancer diseases.

Cannabidiol (CBD) , the main non psychotropic cannabinoid present in Cannabis sativa plant, has emerged in the last decades as potential anticancer drug, due to its ability to inhibit cancer cell proliferation, adhesion, migration and invasion of several kind of tumors such as breast and prostate cancer. Nevertheless, the stability problems of CBD and its high liposolubility, difficult the development of an effective formulation with this compound. Microencapsulation may resolve these questions and also may improve the antitumor activity of CBD. The aim of this work was (i) to determine the antiproliferative effect of CBD in ovarian cancer, using SKOV-3 cell line as model and evaluating the induction of apoptosis and generation of ROS and (ii) to develop biodegradable microparticles (MPs) loaded with CBDfor intraperitoneal administration. SKOV-3 cell viabilitywere determined by MTT assay and apoptosis and ROS generation by flow cytometry. MPs were elaborated by emulsification-evaporation technique, using poly-D, L-lactide-co-glycolide (PLGA) as polymer. CBD demonstrated an antiproliferative effect in SKOV-3 cells, with an inhibitory concentration 50 (IC50) of 21.43µM after 48 hours of incubation, exerting a pro-apoptotic effect. However, the generation was not observed, rather, CBD showed an antioxidant activity. Developed Mps were spherical, showing a non-porous and uniform surface, and a high drug loading and entrapment efficiency. The particle size (expressed as volume dimeter) was of 28.57µm.

M Suñe-Pou has completed his degree in Pharmacy with a special award at the age of 22 years from University of Barcelona (UB). Currently, he has started his PhD studies with an investigation scholarship given by UB. He is working and collaborating in the research group “Transport systems for delivery drugs” in the SDM (Service of Development of Medicines) and with the research group “nRNA formation and function” in the Institute of Parasitology and Biomedicine “Lopez-Neyra” (IPBLN). He has published 4 posters in reputed congresses, one chapter in a book of pharmaceutical technology and has participated in teaching tasks along with the degree.

The Faculty of Pharmacy of the University of Barcelona has a close relationship with pharmaceutical companies and it is very active in the development and transfer of knowledge and technology. The Faculty has in house the facilities to carry out high demanding projects. In particular the Service of Drugs Development and the Laboratory of Medicinal Chemistry conduct uninterruptedly joint projects with pharmaceutical companies. Worthy of note, the outstanding laboratories Esteve, Novartis, Almirall, Cinfa, Salvat, Combinopharm Boerhringer Ingelheim, etc. are travel partners in the discover of solutions in the field of synthesis and development of new drugs. With the aim of illustrating this context two recent shared projects Faculty of Pharmacy-industry, will be considered. One of the projects, developed in the Laboratory of Medicinal Chemistry, concerns the development of a new class of therapeutically active compounds that target the 11-hydroxysteroid dehydrogenase 1 (11-HSD1). The framework of the project carried out in the Service of Drugs Development involves the micro-capsulation of proteins to be orally administrated.

Melania F Munteanu has completed his PhD from University of Medicine and Pharmacy, Targu Mures (Romania). She is a Lecturer of Vasile Goldis West University, Arad (Romania), Health and Environmental Chemistry discipline – Pharmacy Department. She has published more than 20 papers in reputed journals.

Drug delivery system represent an improved method used to deliver many drugs with a higher biodisponibility. Most of these carriers are based on nanoscale particles, tubes, dendrimers, etc. In this study, polyurethane structures with and without 2,4-dinitrochlorobenzene (DNCB, an organic compound used as reference agent to cause contact dermatitis) were synthesized using an interfacial polyaddition combined with a spontaneous emulsification. The obtained nano- and micro-structures were characterized by solubility tests, aqueous solutions’ pH, thermal analysis, SEM, and ultraviolet-visible absorption spectroscopy. The yield of encapsulation of DNCB inside nano- and micro-structures was evaluated using HPLC/MS analysis. Three different sizes of polyurethane structures were obtained: 72±7 nm, 348±12 nm, and 1287±31 nm; the samples were almost homogeneous, with a polydispersity index around 0.2 units, and a medium stability (Zeta potentials around +23 mV). The polymer structures with elongated shapes present a better solubility in organic solvents, and at pH values between 6.1 and 7.3. In vivo evaluations of skin parameters, such as transepidermal water loss, mexametry (assessment of erythema level and melanin content) and corneometry (hydration level of skin surface), were done using SKH1 hairless mice. The results suggest that nanostructures have a similar effect as DNCB which can be associated to a high degree of skin penetrability.

Shayan F Lahiji has completed his BS and MS from Yonsei University (South Korea) and is currently doing his PhD at the same university. Because of his outstanding contribution to science and new novel delivery systems, he has been awarded in different fields of science for “The best poster presenter” from 3rd world biotechnology conference, “The best research award” from Yonsei University and “The best academic poster” from BK21 PLUS Research Symposium and more. He has published papers in reputed journals such as “Scientific Reports” from Nature Publishing Group and “Biomaterials” from Elsevier.

Insulin is a peptide hormone which regulates metabolism of fats and carbohydrates by absorption of glucose. When insulin production of body is inadequate, glucose level of blood increases and results in diabetes. Delivery of insulin is regarded as the most important part of diabetes treatment. Insulin helps body to maintain the necessary blood glucose level and patients must inject prescribed dosages of insulin daily to themselves. Continuous injection of insulin is often uncomfortable for patients and the needle causes injury and pain to the skin. On the other hand, the needle wastes are not environmental friendly and require complex procedure to recycle. Therefore, we developed dissolving microneedles that are capable of delivering insulin upon insertion into the skin. The backbone used to fabricate microneedles was carboxy methyl cellulose (CMC) and Humalog insulin was encapsulated into the microneedles. Previously, dissolving microneedles were fabricated over patches for application. However, we found that patches reduce the insertion rate of microneedles by 60% in normal skins and by 80% in hairy skins. To solve this problem, we also developed a novel micro-pillar based applicator which is capable of inserting microneedles into skin in a minimal invasive manner within less than 1 second. Our data showed up to 97% delivery of insulin encapsulated microneedles, when delivered by micro-pillar applicator.

Anton Aleksashkin has completed his Master’s degree from Lomonosov Moscow State University (MSU). He is a PhD student of Lomonosov MSU in the Faculty of Chemistry and a research fellow in BIND RUS.

Numerous diseases ranging from neurodegenerative to some types of cancers are associated with overproduction of reactive oxygen species. Injection of antioxidants could decrease oxidative stress. Antioxidant enzymes, such as superoxide dismutase (SOD) and catalase, are the most effective antioxidants in nature and could be used to slow oxidative stress. Unfortunately, injection of native enzymes is not effective due to their rapid elimination and instability in blood. Nanoparticles called “nanozymes” based on block-ionomer complexes of negatively charged proteins with positively charged block-copolymers (in particular, polylysine-polyethyleneglycole, PLL-PEG) were previously developed to encapsulate SOD. These cross-linked particles – nanozymes-1 have nanoscale size and preserve specific activity. However, fast release of enzyme from complexes leads to fast elimination from the body. In this presentation, novel type of nanozymes-2 will be discussed. Second negatively charged block-copolymer (poly(glutamic acid)-polyethyleneglycole (PGlu-PEG) was used, and protamine was used instead of PLL-PEG. We were able to increase the reaction yield from 5% to 45%. Developed particles have neutral charge, 50 nm hydrodynamic diameter while nanozymes-1 have slightly positive charge and 40 nm hydrodynamic diameter. Pharmacokinetic experiments showed remarkably increased T1/2 and AUC of double nanozymes versus both standard nanozymes and native SOD. To evaluate therapeutic efficiency of nanozymes, rat spinal cord injury model was used. Recovery of rats was investigated with MRI imaging and BBB-test. Animals that were injected with nanozymes-2, had significant higher scores in BBB-test and lower volume of damage. Thus, easy, scalable method to encapsulate antioxidant enzyme, SOD, was developed.

Ana Mafalda Paiva has completed her PharmD from Pharmacy Faculty, University of Porto. She also has a Master’s degree in Quality Control, from the same institution. Her work led to four papers in peer reviewed journals and several poster presentation at national and international scientific meetings, in the areas of nanotechnology, medicinal and analytical chemistry. She is working as an analytical Chemist now, focusing analytical method development, at Hovione, Portugal.

Dissolution is an analytical test commonly used by the pharmaceutical industry to guide both formulation design and drug product quality control. When considering the development of a dissolution method, two main goals must be considered: 1) ensure consistent lot-to-lot quality for commercial products; 2) be suitable as QC tool for daily routine. The traditional dissolution approach often emphasizes its application in quality control testing and usually strives to obtain 100% drug release. In the presence of two oral granules formulations, with in vivo data available, that showed differences in bioavalability, the initial method development was focused on a traditional dissolution approach. However, results showed that the method used had no disciminatory effect, therefore not reflecting the in vivo data. A biorelevant dissolution method development followed - a pH shift method, where for the initial 30 minutes a low pH was applied followed by 90 minutes of neutral pH, was undertaken. The goal was to mimic the pH differences throughout the gastric system. The pH adjustment had been previously tested to ensure that the addition of NaOH 1M and PBS would shift the pH 1 to pH 7. The development of a robust method, that allowed the correlation with in vivo data was successfully achieved and discrimination between prototypes was accomplished. The current work also shows that with proper development, pH shift dissolution methods can suit early development and routine QC lab needs.

Abdulaziz Mohsen Al-mahallawi, has completed his masters in 2012 from Faculty of Pharmacy, Cairo University, Egypt. He is working at pharmaceutics and industrial pharmacy in the faculty of pharmacy, Cairo University. He is a member in the drug manufacture unit (DMU) in the faculty of pharmacy, Cairo University. He has published 7 papers in reputed journals.

Ciprofloxacin is a broad spectrum fluoroquinolone antibiotic that has been used for systemic treatment of otitis media in adults. In addition, ciprofloxacin was approved for topical treatment of otorrhea in children with tympanostomy tubes. The aim of this work was to enhance the local non-invasive delivery of ciprolfolxacin across an intact tympanic membrane (TM) to the middle ear in an attempt to treat otitis media ototopically. In order to achieve this goal, ciprofloxacin nanovesicles, spanlastics, were prepared by thin film hydration technique technique (TFH ) using several edge activators (EAs) at Span 60: EA weight ratio of 8:2. A full factorial design (32) was employed to optimize formulation variables including; type of EA and Span 60: EA wight ratio using Design-Expert® software. The optimal formulation was then subjected to physical stability studies and ex-vivo permeation studies (through ear skin and TM of rabbits). Results revealed that the optimal formulation (composed of Spna 60 and Brij 35 as an EA at a weight ratio of 8:2) exhibited enhanced ex-vivo drug flux through ear skin and TM when compared with the commercial product (Ciprocin® drops). It also exhibited good physical stability after storage in refrigerator (4-8 °C) for six month, as the physical properties of this formulation (appearance, drug content, entrapment efficiency, particle size, polydispersity index, and zeta potential) did not significantly change after storage in the specified conditions. Consequently, spanlastics could be promising nano-carriers for the non-invasive trans-tympanic delivery of ciprofloxacin.

Loco-regional delivery of Tamoxifen Citrate (TMC) is used in this study to localize its activity into the vicinity of tumor and hence improving therapeutic outcome with less toxicity on other organs. Herein, innovative TMC niosomal thermosensitive gels were proposed as a tool to achieve this goal. Niosomes were prepared by thin lipid film hydration technique and evaluated for cellular uptake and cytotoxicity. The anti-cancer activity was also tested in vitro using MCF-7 breast cancer cell line. Moreover, in vivo anti-tumor efficacy was examined in Ehrlich carcinoma mice model through reporting solid tumor volume regression and tissue TMC distribution. Significantly enhanced cellular uptake (2.8 fold) and greater cytotoxic activity with MCF-7 breast cancer cell line were obtained from vesicles prepared with span 60: cholesterol (1:1 molar ratio). Niosomes were then packed in thermosensitive gels using cold method. TMC niosomal thermosensitive gels were evaluated for gelation temperature, rheological behavior and in vitro drug release. Type and ratio of used poloxamers were manipulated to provide an optimal gelation temperature (34-37°C). Rheological analysis showed low viscosity and elasticity values at low temperature while these values significantly increased at elevated physiological temperature. A prolonged release of TMC following a diffusion-driven release model was detected. Furthermore, in vivo data showed evidently that anticancer activity was improved with significant retention of the drug at the tumor site. These encouraging results confined that this in situ gel depot offers an attractive approach for controlled delivery of TMC and clinically expected to be useful candidate in breast cancer loco-regional therapy.

Dalia Samuel Shaker is a Professor of Pharmaceutics at the College of Pharmacy, Future University, Cairo, Egypt. She has twenty years of academic and industrial experience in Pharmaceutical Sciences; her Doctoral research was performed at the University of Utah, USA with Prof. William I. Higuchi on transdermal drug delivery using radioactive permeants, permeation promoters and chemical enhancers. Her Postdoctorate research was conducted at Oregon State University, Corvallis, Oregon, USA, on transdermal vaccines. Her research has resulted in twenty seven publications in international journals and fourteen presentations at international conferences. She is a Editorial Board Member of of Future Journal of Pharmaceutical Sciences.

Ahmed R Fares has completed his Master degree in pharmaceutical sciences from faculty of pharmacy, Cairo University. He is now a Phd student in the same University. He is a teaching assisstant in the pharmaceutics and industrial pharmacy department. He has published 2 papers in reputed journals.

Lacidipine (LCDP) is a calcium channel blocker used in the treatment of hypertension. However, LCDP is a highly lipophilic drug of poor aqueous solubility which leads to poor absorption upon oral administration. The aim of this study was to prepare and optimize LCDP nanosuspensions using the antisolvent sonoprecipitation technique to enhance the solubility, dissolution and oral absorption of LCDP. A three factor, three level Box-Behnken design (BBD) was employed to optimize the formulation variables to obtain LCDP nanosuspension of small and uniform particle size. Formulation variables included in the design were: stabilizer to drug ratio (A), sodium deoxycholate (SDC) percentage [a mixture of SDC /Pluronic F127] (B) and sonication time (C). LCDP nanosuspensions were assessed for particle size (PS), zeta potential (ZP) and polydispersity index (PDI). The formula with the highest desirability (0.969) was chosen as the optimized formula. The values of the formulation variables (A, B and C) in the optimized nanosuspension were 1.5, 100% and 8 min, respectively. The optimal LCDP nanosuspension was lyophilized using 2% mannitol as cryoprotectant. The X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) studies showed amorphous LCDP nanoparticles. Transmission electron microscopy (TEM) demonstrated spherical particle morphology. LCDP nanosuspension showed significantly enhanced saturated solubility and dissolution rate in comparison to raw LCDP due to particle size reduction and amorphous state. These results suggest that the optimized LCDP nanosuspension could be promising to improve oral absorption of LCDP.

Maja Szczepańska is the first year PhD student at the Medical University of Gdańsk, Poland. She completed her Master’s degree in Pharmaceutical Sciences in 2014. She is working on her PhD thesis at the technology of minitablets. The aim of her work is to optimize the coating process of minitablets and develop a method for testing the release rate from coated minitablets.

Minitablets (MT) are innovative solid oral forms designed especially for pediatric and geriatric patients with swallowing problems. MT (diameter 1-3 mm) are regarded as a multiple unit dosage forms, same as granules or pellets, where the dose is administered as a variable number of subunits. Multiple unit dosage with controlled release carry lower risk of uncontroled burst release of the drug. Minitablets are alternative for pellets because of their ease of preparation. Due to the defined sizes, weight and smooth surface minitablets are produced in a more reproducible and continuous way. The aim of the study was to develop minitablets (2.5 mm cores) with prolonged release, where carbamazepine (CBZ) was a model drug. Modified release was achieved by fluid bed coating. Two series of minitablets containing 25% of CBZ were prepared; by direct compression (MT-DC) or by compression after granulation (MT-GR). Rotary tablet press (Erweka RTP-D8, Germany) was used. MT were coated in fluid bed system (Aircoater 025, Innojet) using a mixture of aqueous dispersions of Eudragit RL and RS polymers at various ratios. The dissolution rate was modified by film thickness and addition of pore forming polymers. Prolonged release of CBZ was achieved for MT-GR with 1:1 Eudragit RL/RS ratio (50 µm film thickness), whereas for MT-DC coated with 1:9 Eudragit RL/RS ratio (30 µm film thickness) drug release rate was found optimal. The drug release profiles of MT complied with the USP requirements for prolonged release tablets. Addition of the pore forming polymers (hypromellose, polyvidone) allowed to eliminate the initial delay in the active substance release.

Peptide conjugates containing somatostatin (SST) cyclic analogs as a targeting moiety are able to deliver chemotherapeutic agents specifically to cancer cells expressing SST receptors, thereby increasing their local efficacy while limiting the peripheral toxicity. Here, we report on the synthesis and biochemical characterization of new SSTR specific anticancer peptide conjugates, with different anticancer payload acting through different oncogenic mechanisms in order to evaluate their biological activities and to provide a comparative study of their drug release profiles. The SSTR2 specific backbone cyclic peptide 3207-86 was chosen for the synthesis of a variety of novel anticancer drug conjugates with a broad drug release capabilities. The N-terminus of 3207-86 was equipped with GABA in order to generate free amino group available for conjugation of Chlorambucil (CLB), Camptothecin (CPT), Combretastatin 4A (COMB), ABT-751 (ABT) and Amonafide (AM) through formation of various biodegradable bonds. The chemo- and biostability/drug release of all the synthetic compounds was investigated at various pHs and in the presence of mouse liver homogenate respectively. Their selective cytotoxic effect was evaluated on several human cancer cell lines that over express SSTR2. Compared with the free drugs, our peptide-drug conjugates exhibited considerable cytotoxic effect on cancer cell lines vs. low SSTR2 expressed HEK cells. Functional versatility of the conjugates was reflected in the variability of their drug release profiles, while the conserved sequence of a selective binding to the SSTR2 likely preserved their binding to the receptor and consequently their favorable toxicity towards targeted cancer cells.

Compact carriers for peptidyl delivery systems (PDSs) loaded with various drugs were synthesized using a simple and convenient solid phase organic synthesis (SPOS) strategy, including semi-orthogonal functional group protection schemes. Each attachment point of the compact carrier can thus be bound to an anticancer agent through a biodegradable covalent link. Chemo- and bio-stability experiments of a model peptidyl platform loaded with 3 different drugs revealed pH and liver homogenate (metabolic) dependent sequential release behavior. The versatility of this approach will serve to expedite the preparation of PDS libraries. This approach may prove useful for applications suitable for personalized medicine where multiple drug delivery is required in a sequential and controlled fashion.

Bazylevich A is a PhD student in Ariel University.

The fundamental problem of present-day chemotherapy is caused by grave side effects of drugs which greatly impair the life quality of patients, and often lead to the therapy cessation. Targeted delivery of a drug into a cancer cell may resolve this issue, which is known and studied extensively all over the world. The anti-tumor drugs employed here, such as trimelamol, amonafide, azatoxin, procarbazine, tubulisine and some substances of natural origin (capsaicinoids and curcuminoids), are currently used in clinics or undergoing clinical trials. It was decided to synthesize platforms loaded with specified drugs. These platforms are based on amino acids or other compounds of natural origin containing multiple functional groups such as flavonoids or polyphenols. Those platforms have been obtained by means of the simple and convenient orthogonally protective solid-phase organic synthesis (SPOS). Each branch of the platform carries a different anticancer agent linked by a bond such as amide, ester, carbamate, or thiourea, thus providing discrete chemo- and bio-release profiles for each drug.

Rania Hamed has received her Ph.D. in Pharmaceutical Sciences from The University of Iowa in 2011. She is currently an Assistant Prof. in the Faculty of Pharmacy at Al-Zaytoonah University of Jordan. Her current research focuses on developing controlled release matrix tablets using hydrophilic/hydrophobic polymers, correlating the rheological properties of the nanoemulsion-based gel formulations to the in vitro permeation of drug molecules, and determining the key parameters of the biorelevant dissolution media that control the rate of dissolution of BCS class II drugs to better predict the in vivo performance.

Drug release from hydrophilic Matrix Tablets (MT) is controlled by the diffusion of the drug through a polymeric gel layer. When MT hydrates, a gel layer is formed. The objective of this study was to examine the utility of controlled-stress rheometer as a novel approach to measure the rheological properties of the gel layer of swollen matrices formed upon tablet hydration. MT were prepared using the low (K100LV) and high (K4M) viscosity grade Hydroxypropyl Methylcellulose (HPMC). Two sets of MT were prepared containing 21.3% K100LV (K100LV MT) and 21.3% K4M (K4M MT). Oscillatory rheological analysis of the hydrated swollen MT was performed using a controlled-stress rheometer. The gel layer exhibited more elastic behavior, where the elastic modulus (G’) dominated the viscous modulus (G”), which is typical for gel materials. Swollen K100LV MT exhibited higher G’ and G” values compared to those of K4M MT. K100LV MT exhibited a lower water penetration and hydration capacity into the matrix compared to K4M MT, resulting in the formation of a thin gel layer. Therefore, the rheological properties of the dry (un-wetted) core of the K100LV MT rather than the thin gel layer were detected. These results suggested that water penetration through MT and extent of hydration depend on the polymer viscosity grade, thereby controlling the formation of the gel layer. Rheological analysis of the gel layer provides a good prediction of matrix hydration from controlled-release MT, which can guide the selection of an appropriate polymer for successful preparation of swellable hydrophilic MT.

Şennur Görgülü Kahyaoğlu has completed her MSc degree from Anadolu University Department of Advanced Technologies-Biotechnology and continue doctoral studies at the same university Graduate School of Health Sciences, Department of Pharmacology. She is responsible for xCELLigence RTCA MP system, flow cytometer, confocal microscope and cell culture laboratory. She is study on nano-biotechnology for novel drug research and development. She has 3 papers in refereed journals and has attended more than 15 conferences.

Pancreatic cancer is one of the worst mortality and malignant types of cancer to treat which has poor diagnose at an early stage, associated with debilitating symptoms and poor prognosis with an aggressive metastasis. Disadvantages of antibody based drug delivery systems are short term and less effective availability because of their brittle structures. Therefore, the development of novel and effective drugs as specific targeted drugs is crucial. Multifunctional magnetic nanoparticles were used for target orientation as a drug carrier. In this study, bioconjugated nanolactoferrin (BCNanoLf) was designed as a new generation polymeric drug carrier system. The bioconjugates were prepared by using ANADOLUCA method that is a cross-linking polymerization technique. Anti-mesothelin antibody and FeCl3 were oriented and cross-linked, Gambogic acid, the natural compound extracted from gamboges as a potent anticancer agent was conjugated to BCNanoLf. This multifunctional nanostructures can be targeted to pancreatic carcinoma cells. Cytotoxicity analyses were performed by xCELLigence real time cell analyzing system for calculation of IC50 values of the bioconjugates. Then flow cytometry and molecular biological analyses were evaluated for in vitro characterization of the bioconjugates. The obtained results in this study showed that the prepared bioconjugates could be used as a potential theranostic drug.

Mohamed Abouleish worked in the environmental industry at an instrumental company (Shimadzu in USA), and taught chemistry and environmental science at several universities, including Tennessee Technological University. His areas of research and teaching interest are environmental protection and management; policies and regulations; water, wastewater, drinking water and pharmaceutical water; solid waste and wastewater treatment; environmental trace analysis; environmental ethics, risk and social issues; and sustainability.

Antibiotics are provided to patients in different forms, e.g. powder, pills, solution. Oral powder antibiotics require water for reconstitution. Pre-packaged water is sometimes provided with antibiotics for reconstitution and at other times it is not provided. When pre-packaged water is not provided, pharmacists recommend the usage of distilled water for reconstitution. Many types of water exist for different uses. Pharmaceutical processes require different types of water, depending on usage, e.g. water for injection, purified water, and highly purified water. Other water types include mineral, spring, drinking, filtered, and distilled water. Many different types of water and different interpretation of the associated terms exist, depending on background and geographical location of the individual. Patients are not aware of the differences in types of water and differences in the terms used, and this creates confusion over which water is appropriate for reconstitution of the antibiotics. In addition, usage of not pre-packaged water for reconstitution may present some issues, as the water used may contain contaminants that exceed specific limits, and as a result may lead to health problems, that the antibiotic may be mistakenly blamed for, and as a result, the patient would be advised to stop using the antibiotics. The results of this study reflect on the quality of water that may be used for reconstitution of antibiotics, and the possible health effects. The research also calls for the need for providing pre-packaged water with all antibiotics that require water for reconstitution, to avoid any confusion and health issues.

Mohamed Haider has completed his PhD at the age of 30 years from College of Pharmacy, University of Maryland and postdoctoral studies from Department of Bioemdical Engineering, Johns Hopkins University. He is an associate professor currently woking at the College of Pharnacy, University of Sharjah, UAE. He has published more than 15 research and review articles and book chapters and has been serving as a reviewer for many reputable journals.

Diltiazem hydrochloride (DTZ HCl) buccoadhesive controlled-release discs for buccal delivery were developed to prolong the drug release and enhance its bioavailability by evading the first pass metabolism. DTZ HCl buccal mucoadhesive discs were prepared by direct compression of mucoadhesive polymers, namely; polyvinylpyrrolidone (PVP K-30), sodium carboxymethyl cellulose (SCMC) and Carbopol 934 (CP934) in combination with Eudragit L100-55, or sodium alginate (SA), as matrix polymers to control the drug release. In vitro characterization of the prepared discs showed that drug release, swelling capacity, surface pH and mucoadhesion depend on the type of mucoadhesive and matrix polymers and their ratios. Further, in vivo testing of mucoadhesion time and acceptability were performed in human subjects. The majority of the developed formulations presented suitable adhesion and controlled drug release. Discs formulae containing SA and SCMC mixtures showed superior properties in terms of ease of preparation, optimum drug release and excellent mucoadhesion values. In addition, subjective parameters and mucoadhesive behavior in healthy human volunteers were found to be more satisfactory. Relative bioavailability of a selected DTZ HCl buccoadhesive formulation (SA/SCMC, 3:1) was determined and compared with that of a commercial sustained release oral tablet (Altiazem® SR) as a reference in rabbits. The percentage relative bioavailability of DTZ HCl from the selected buccal mucoadhesive disc was found to be 197.7%. The estimated tmax and AUC0-∞ values were also significantly higher after buccal administration (p <0.05). The proposed buccal buccoadhesive formulation of DTZ HCl could be an alternative for the currently available oral therapy.

A Zaidalkilani is an Assistant Professor at faculty of Pharmacy, Zarqa University, Zarqa, Jordan. Now, she is a head of pharmaceutical science department. She completed her PhD in drug delivery and pharmaceutical technology at the Faculty of Pharmacy, Queen’s University of Belfast, Belfast, United Kingdom in October 2013. She has published more than 6 papers in reputed journals.

The poor oral bioavailability of proteins requires that they be administered mainly by parenteral routes. Moreover, the short plasma half-lives of these drugs means they typically require repeated injection, leading to poor patient compliance. These factors have lead to the search for novel delivery methods, such as transdermal administration through intact skin. Skin is an appealing site for systemic delivery of active pharmaceutical ingredients. However, the stratum corneum, which is the outermost layer of the skin, acts as the principal barrier for penetration of most drugs. Therefore, microneedle (MN) arrays will be combined with iontophoresis (IP) in order to enhance delivery of drugs across the skin. The primary aim of this study was to evaluate the ability of super swelling hydrogel MN arrays coupled with IP to facilitate the transdermal delivery of a model protein, OVA from electro-responsive patch. Super swelling hydrogel forming MN arrays, containing aqueous blends of 20% w/w Gantrez® S97 and 7.5% w/w PEG 10,000 were prepared by diluting the 40% w/w Gantrez® S97 stock solution and mixing it with the required amount of PEG 10,000 solution and subsequently 3% w/w Na2CO3 added. Electro-responsive patches containing OVA were prepared using a casting method, from aqueous blends containing 10% w/w Gantrez® AN139 and 5% w/w tripropylene glycol methyl ether (TPM). The drug reservoir film mediated electrically responsive drug delivery was physically and electrically characterized using a suite of techniques, such as thermal analysis (mDSC), tensile testing (texture analyzer). Altering patch formulation e.g. changing the casting gel pH produced substantial alteration in physicochemical properties of films. The feasibility of super swelling hydrogel MN arrays to deliver OVA form electro-responsive patch was evaluated in vitro. In vitro OVA delivery experiments were performed using the Franz cell apparatus. All samples were analysed using ELISA. The in vitro OVA permeation experiments indicated that super swelling hydrogel MN arrays with electro-responsive OVA loaded patch capable of providing a sustained transdermal OVA delivery over a 24 hours period. Furthermore, the synergistic effect of MN and iontophoresis arrays led a two-fold enhancement in the cumulative amount of insulin permeating across neonatal porcine skin after 6 hours. In addition, it was found that the electrically responsive nature of these super swelling hydrogel MN and patches led to a dramatic increase in OVA transport when such systems were combined with IP.

Rania Hamed has received her PhD in Pharmaceutical Sciences from The University of Iowa in 2011. She is currently an Assistant Professor in the Faculty of Pharmacy at Al-Zaytoonah University of Jordan. Her current research focuses on developing controlled release matrix tablets using hydrophilic/hydrophobic polymers, correlating the rheological properties of the nanoemulsion-based gel formulations to the in vitro permeation of drug molecules, and determining the key parameters of the biorelevant dissolution media that control the rate of dissolution of BCS class II drugs to better predict the in vivo performance.

Dissolution of the BCS class II is dependent on the Gastrointestinal (GI) physiological factors. Surface Tension (ST) is a major characteristic of the GI fluids that can affect drug release rate. Typical ST values of the gastric and intestinal fluids are in the range of 30-45 and 28.8-32.3 mN/m, respectively. Carvedilol, a weakly basic BCS II drug, was used as a model drug. Due to its poor aqueous solubility, carvedilol exhibits very low bioavailability and may precipitate upon entry into the small intestine. The objective of this work was to study the effect of the ST of GI fluid on carvedilol release rate to better understand the dissolution and precipitation behaviors of weakly basic drugs. Dissolution media that simulate the gastric and intestinal fluids with and without the anionic surfactant Sodium Lauryl Sulfate (SLS) were used in this study. The ST of the dissolution media was measured using the du Noüy ring method. The rate of carvedilol release from Dilatrend® tablets was investigated using dissolution type II apparatus. The addition of SLS to gastric and intestinal fluids lowered the ST from 39.5±2.5 to 27.8±3.2 and from 62.9±5.5 to 31.9±2.6 mN/m, respectively. The rate of carvedilol release in gastric and intestinal fluids was significantly enhanced upon the addition of SLS. As the ST of the dissolution media decreases, the percent of carvedilol released increased. Simulating the ST of the compendial GI fluids could improve our knowledge of the dissolution, precipitation behavior, and in vitro-in vivo correlations of the weakly basic drugs.

Bahar Demir has graduated from EskiÅŸehir Osmangazi University Department of Biology. She is doing her Post-graduation at Anadolu University Department of Biochemistry. She is studying on anti-cancer agents for novel drug research and development. She has taken part in 2 projects and has attended more than 5 conferences.

Cancer is the second leading mortality cause all over the world. Treatments againsts cancer are drugs (chemotherapy), surgery, radiation and/or immunotherapy. However, an effective drug for therapy and prognosis after surgery still do not exist. Therefore, an effective new drug development process is seemed to be necessary. Pyrimidine ring is the building unit of DNA and RNA and thus pyrimidine based chemical architectures exhibit diverse pharmacological activities. Among the reported medicinal attributes of pyrimidines, anticancer activity is the most extensively reported . In this study, we aimed to investigate the cytotoxic and apoptotic properties of series of novel pyrimidine derivatives bearing various heterocyclic rings against A549 cells. A549 lung adenocarcinoma cell lines were used in the studies. The cytotoxic activities of the tested compounds were determined by cell proliferation analysis using standard (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Detection of apoptosis was performed using Annexin V-FITC apoptosis detection kit BD, Pharmingen according to the manufacturer’s instruction. All measurements were performed on a BD FACS Aria (I) cell sorter cytometer. The IC50 values of N’-(arylidene)-2-[(pyrimidine-5-yl)thio]acetohydrazide derivatives (1-12) were determined for A549 cell lines. Compounds 1, 2 and 9 which were including 2-pyridyl, 3-pyridyl and naphtyl moieties, had significant cytotoxic activity with IC50 values lower than 213.3±32.15 μg/mL. Compound 9 showed the highest cytotoxic activity with a IC50 value of 21.00±1.41 μg/mL, whereas, cisplatin IC50 values were 16.33±1.53 μg/mL against A549 cells. Compound 1 showed the highest population of early and late apoptotic cells (19.7%) of the tested compounds which was 3.94-fold higher than for cisplatin. Compound 2 and 9 did not induce apoptotic cell death. It was determined that synthesized compounds 1, 2 and 9 had considerable cytotoxic effects against A549 cell lines compared to cisplatin. Our study results demonstrated that compound 1 namely N’-(2-pyrilidene)-2-[(pyrimidine-5-yl)thio]acetohydrazide affected A549 cells by the apoptotic pathway. Also was evaluated LOX inhibition activity on compounds.

JustÄ— BaranauskaitÄ— has started her PhD of biomedical sciences at the age of 24 in Lithuanian University of Health Sciences right after the graduation. She worked as a scientist in the Analytical chemistry and toxicology ever since. She has published 1 paper in reputed journal, participated in many conferences.

Oregano is an aromatic plant widespread in Mediterranean countries and it is rich in phenolic compounds with powerful antibacterial and antifungal properties. However, there are some difficulties for the storage of the flavor compounds due to the growth of microorganisms. Spray-drying technology provides several benefits to protect ingredients that are sensitive to light, oxygen and free radical degradation. The aim of this study was to prepare microparticles by using different concentration of wall materials (gum arabic and maltodextrin) and to select the best combination of matrix structure to be used as an encapsulating agent through analyses of the physicomechanical properties of the produced microparticles. The optimal conditions were maintained based on the yields of ursolic, rosmarinic acids and carvacrol. The experimental design of two – components system is conducted by using Design Expert. The resulting mixtures were homogenized in a magnetic stirrer, maintained at 25oC for 1 hour and subjected to spray drying. The ratio of wall material and oregano extract was 2:1, wall material concentration was 10%. The powders were obtained using Mini Spray Dryer and was used with vacuum of 6 mBar and aspiration 100%, the inlet temperature was 180ºC and outlet temperature depended on the inlet temperature, feed flow rate was 30 mL/min. For determination of ursolic acid, rosmarinic acid and carvacrol were using UPLC analysis. The results showed that the wall material matrix concentration of maltodextrin 8.74% and gum arabic 1.26% were the optimized conditions for spray-drying oregano ethanolic extract when all significant response variables were compared using the desirability function.

Ugnė Čižauskaitė has started her PhD of biomedical sciences at the age of 23 in Lithuanian University of Health Sciences right after the graduation. She worked as a scientist in the Drug technology laboratory ever since. She has published 1 paper in reputed journal, participated in many conferences.

Nowadays, novel topical formulations loaded with natural functional actives are under intense investigations. We noticed that using low emulsifier (complex of sodium polyacrylate and polysorbate 20) concentration (0.5%) rosemary extract intends to form water/oil/water (w/o/w) type multiple emulsion directly, no additional ingredients or technological stage required. Addition of rosemary extract and some of its active ingredients (rosemarinic (RA), oleanolic (OA) and ursolic acid (UA)) into emulsion formulation had a significant influence on its parameters such as creaming index (CI), spreadability and dispersive phase dropplet size.We decided to investigate if this effect occurs due to the surface and interfacial tension change caused by UA and OA that are saponins. The surface tension measurements were made using the Du-Noüy ring taking into account the Zuidema Waters correction. Rheology modifier used to form emulsion decreased the surface tension of olive oil by 4.96%, of liquid paraffin - by 3.78% (p<0.05). We can hypothesize, that it is the reason why olive oil emulsions are more stable then those with liquid paraffin. The interfacial tension between ethanol (90%) – liquid paraffin and ethanolic rosemary extract-liquid paraffin differed insignificantly, though with vegetable oil the interfacial tension with ethanolic extract was 16.5% lower (p<0.05 vs ethanol (90%)). All the other tested solutions of active ingredients from rosemary extract had no influence on the interfacial tension with olive oil. So we can conclude that the investigated active ingredients (RA, OA, UA) of rosemary extract did not decrease the interfacial tension as it was expected, therefore their emulsion stabilizing effect is not surfactant-like.

Hafiz Makeen is an Assistant Professor in the Department of Clinical Pharmacy, College of Pharmacy, Jazan University, Saudi Arabia. Dr. Makeen has completed his PhD in cancer therapeutics in 2012 from the University of Bradford, United Kingdom. He has completed his master degree in clinical pharmacy in 2002 from the college of pharmacy, King Saud University, Riyadh, Saudi Arabia. Currently he is the Vice Dean for clinical affairs at the college of pharmacy, Jazan University, KSA. Dr. Makeen's area of research in addition to clinical pharmacy is cancer research and the drug delivery to solid tumors.

Chemotherapy is one of the treatment options for cancer. A major problem in cancer chemotherapy is the lack of selective toxicity of many commonly used anti-cancer agents towards tumor tissue compared to normal tissue. Studies have shown that α-naphthol is selectively toxic to cultures of human tumor tissue compared to normal tissues in vitro. Hence, this study was conducted to synthesize a series of new hydroxamate derivatives containing α-naphthol nucleus by the reaction of naphthol acetic acid with amino acid methyl ester derivatives which were directly reacted with hydroxyl amine at room temperature. Structures of these compounds were confirmed by standard studies of IR, 1H-NMR, 13C-NMR, MS and elemental analysis. The cytotoxicity of the synthesized compounds were studied using the MTT assay in four human cancer cell lines, including HepG2, PC-3, HT-29 and MCF-7. Among the compounds, N-hydroxy-2-(2-(naphthalen-1-yloxy) acetamido)-3-phenylpropanamide; had exhibited significant cytotoxicity against almost all the used cells including the normal cells (WRL-68). N-hydroxy-3-(4-hydroxyphenyl)-2-(2-(naphthalen-1-yloxy) acetamido) propanamide; has shown cytotoxicity to HepG2 cells alone with an IC50 of 12.17 µg/ml. The next significant compound which showed cytotoxicity was (N1-hydroxy-2-(2-(naphthalen-1-yloxy) acetamido) pentanediamide. Further studies have shown that the cell death observed was closely associated with generation of reactive oxygen species (ROS). In this study, other napthol derivatives have shown significant increase in the level of ROS in concentration dependent manner in treated cells. In conclusion, the study has shown that among the synthesized compounds, ((N-hydroxy-2-(2-(naphthalen-1-yloxy)acetamido)-3-phenylpropanamide; and (N-hydroxy-3-(4-hydroxyphenyl)-2-(2-(naphthalen-1-yloxy) acetamido) propanamide; hold the potential for further research.

Nehal has got her Master’s degree in Pharmaceutical Chemistry from the German University in Cairo in 2015. She is currently working as a Research Assistant in Zewail City of Science and Technology. Moreover, Nehal is a Drug Design Ph.D. student in Zewail City. She has 2 publications in reputable international journals as well as an accepted Poster in another international conference.

Tamoxifen (TAM) is a widely used drug in the prophylaxis and treatment of breast cancer. TAM is metabolized to the more active 4-hydroxytamoxifen (4-OH-TAM) and endoxifen by cytochrome P450 (CYP) mainly CYP2D6 and CYP3A4 enzymes. Due to the genetic polymorphisms in CYP2D6 genes, high variation in the clinical outcomes of TAM treatment is observed among women of different populations. To address this issue, novel TAM analogues with possible altered activation pathways were synthesized. These analogues were tested for their antiproliferative action on MCF-7 breast cancer cell lines as well as their binding affinity for estrogen receptor (ER) ER-α and ER-β receptors. These entire novel compounds showed better antiproliferative activity than did TAM on the MCF-7 cells. Moreover, compound 1 exhibited a half maximal growth inhibition (GI50) that was 1000 times more potent than that of TAM (GI50 <0.005μM vs 1.58 μM, respectively). Along with a broad spectrum activity on various cancer cell lines, all the TAM analogues showed considerable activity on the ER-negative breast cancer cell line. For further study, compound 2 was incubated in human liver microsomes (HLM), human hepatocytes (hHEP) and CYP2D6 supersomes. The active hydroxyl metabolite was detected after incubation in HLM only, implicating the involvement of other enzymes in its metabolism. These results prove that this novel series of TAM analogues might provide improved clinical outcomes for poor 2D6 metabolizers.

Marc Suñé Pou has completed degree in Pharmacy with a special award at the age of 22 years from University of Barcelona (UB). Currently, he has started his PhD studies with an investigation scholarship given by UB. He is working and collaborating in the research group “Transport systems for delivery drugs” in the SDM (Service of Development of Medicines) and with the research group “nRNA formation and function” in the Institute of Parasitology and Biomedicine “Lopez-Neyra” (IPBLN). He has published 4 posters in reputed congresses, one chapter in a book of pharmaceutical technology and he has participated in teaching tasks along the degree.

SeDeM Diagram System is a new Galenic method for application in tablet-preformulation and formulation studies. It provides information about the suitability of active ingredients and excipients in powder for direct compression. Moreover, this useful tool is also apt for verification of the reproducibility of manufacturing standards between batches of the same powdered raw material (API or excipient). Indeed, superposing the SeDeM Diagrams of each batch, the degree of similarity or difference between the same API on the basis of the established twelve physic parameters can determine its appropriateness for compression. It is widely known that one substance, with exactly the same chemical structure, can vary his physical characteristics depending on the provider and the trademark. Consequently, there have been in many occasions unexpected problems in manufacturing process of drug products. Two batches from the same API (Aspirine) and provider are compared in order to demonstrate the differences between different batches of the same provider of the same chemical product. The two SeDeM Diagrams are represented and compared, allowing us to study the differences between two batches easily. Also, it allows to know quickly if the batches are good enough for direct compression, and to correct the powder properties that need to be improved to facilitate the formulation of the end product for direct compression of this API.