9^th World Drug Delivery Summit June 30-July 02, 2016 New Orleans, Louisiana, USA

Mark Pothecary studied biochemistry at the University of Bath before getting his PhD at the William Harvey Research Institute, part of the Queen Mary University. He joined Malvern in February 2008 at a technical specialist for DLS and GPC/SEC in the UK and is now the Product Manager for GPC/SEC products in the Americas.

Poly(D,L-lactide-co-glycolic acid), PLGA, is a copolymer of polylactic acid and polyglycolide. As a biodegradable and biocompatible polymer, it is has found use in a number of medical devices such as grafts and sutures as well as in drug delivery applications. Drug delivery profiles will be dependent on the molecular weight, composition and structure of the polymer. Gel-permeation chromatography (GPC) is the most widely used tool for the measurement of molecular weight and molecular weight distribution of natural and synthetic polymers. Static light scattering detectors measure the intensity of light scattered by the sample as it elutes from the column. Since the intensity of the scattered light is proportional to the sample’s molecular weight and concentration, they allow the direct measurement of the sample molecular weight independent of its elution volume. A viscosity detector can also be used as part of a GPC system to measure the parameter of intrinsic viscosity. In combination these data allow detailed structural information of a polymer to be generated in a single GPC measurement which can be compared with other samples in Mark-Houwink plots. In this paper, we analysed different samples of commercially available PLGA to compare their absolute molecular weight from light scattering to those quoted with the product using Malvern’s latest GPC/SEC system, OMNISEC. Structural differences between samples of different composition are clear. More detailed analysis of these parameters can be used to better control the end-properties of the PLGA and its release rate of drugs in delivery applications.

Alexandre Samoylov has received his PhD in Molecular Biology at the age of 27 years from the Institute of Molecular Biology (Kiev, Ukrane). He has completed postdoctoral studies at the DLO-Center for Plant Breeding and Reproduction Research (Netherlands) and at the Institute of Plant Genetics & Crop Plant Research (Germany). At present, he holds a Research Fellow IV position at the Scott-Ritchey Research Center Auburn University College of Veterinary Medicine (USA). He has published more than 40 papers in peer-reviewed journals. His current focus is on development of phage- and DNA-based vaccines for animals.

DNA vaccination is achieved by injecting an animal with genetically engineered DNA to stimulate antigen-specific immunological responses. One of the greatest advantages of DNA vaccines is that they are able to activate both arms of the immune system, humoral and cell-mediated. Potency of DNA vaccines can be increased drastically (hundreds of times) via advanced delivery methods. Even though muscle was the first and is the most traditional site for DNA injections, skin was shown to be an immunologically superior site for DNA immunization due to abundant presence of immune cells such as Langerhans and dendritic cells. This study reports the development of DNA-based contraceptive vaccines constructed to stimulate effective immune responses against pituitary cells expressing gonadotropin releasing hormone receptors (GnRHR). Two delivery routes for the constructed vaccines were tested in mice, 1) intramuscular injection into quadriceps muscle, and 2) intradermal injection of the ear pinna. Inoculation of the ear pinna, but not intramuscular injection, was shown to stimulate immune responses leading to suppression of testosterone (indirect indicator of the vaccine efficacy) and decreased expression of GnRHR mRNA that might be due to partial ablation of pituitary gonadotropes expressing GnRH receptors. The success of the intradermal delivery might be explained by the special structure of the pinna, which consists of two layers of epidermis and dermis (separated by ear cartilage) containing a high number of dendritic cells (most effective APCs) within a restricted area connected with major superficial cervical draining lymph nodes. Funded by Found Animals Foundation, Michelson Grant in Reproductive Biology D1213-F13.

Terence James Noonan completed his B.Pharm degree at the North-West University’s Potchefstroom campus in 2010, an M.Sc in pharmaceutics in 2012 and is currently enrolled as a PhD candidate at the University of Cape Town.

Pharmacologically active drug leads are often pre-emptively rejected at an early stage of development if they display undesirable physicochemical properties. The aim of synthesising new solid-state forms of drugs through supramolecular derivatisation is to alter their properties while maintaining their pharmacological activity. This is achieved by the formation of non-covalent bonds with biocompatible partner molecules (in co-crystals, salts, inclusion complexes, solvates or hydrates) or by altering the way in which these molecules are arranged and interact within their various polymorphic crystals. These new forms can have significantly different values for their dissolution rates, processability, or physical and/or chemical stability, which can translate into positive effects such as reduced doses required for the same effect, longer shelf-life and reduced side-effects, among many others.1, 2 An antimalarial drug lead which displayed good in vitro potency (IC50: K1 = 6.3 nM, NF54 = 7.3 nM) against multidrug resistant (K1) and sensitive (NF54) plasmodial strains and exhibited 98% activity in the in vivo Plasmodium berghei mouse model in a 4-day test at 4 × 50 mg/ kg po, showed poor aqueous solubility (<5 μM at pH 6.5).3, 4 New crystal forms of the drug lead were created in an attempt to overcome this inadequacy. We report novel co-crystals, polymorphic forms and a hydrated form of this new drug candidate. Their characterization was performed using X-ray diffraction, hot stage microscopy and differential scanning calorimetry. Future work is aimed at assessing these forms in terms of solubility, dissolution rate and bioavailability through studies in animal models.

Serrano Mora Is 26 years old, he had completed his Bachelor degree in Chemistry at the age 23 years from UNAM. Currently he is studing a master in chemistry science his project is about coprocessed material to be used in controlled release of drugs, his superviser is the professor David Quintanar Guerrero.

Nowdays, there is a growing interest to search new formulation materials capable to release drugs in a controlled way with less manufacturing process steps. These materials need to have improved properties in relation with the conventional raw materials such as to reduce manufacture costs, to add functionality to the dosage form, to have compatibility with all active substances and to be safe for a specific administration route. Thus, it is recognized the importance of the excipients more than ever, in particular those with additional activities or functions. In the case of a functional excipient for direct compression must provide high flow, excelllent capacity to form uniform mixtures and good compressibility among others. To increase the use of the direct compression in the pharmaceutic tableting are needed novel excipients which can be easily adaptable to formulate different drugs. However, this is not an easy task so while more compressible is a material lesser fluid. The technology more profitable is improved the functionality of a existing excipient using new techniques of procesing or combined in a synergistic way two or more excipients in order to form coprocessed materials. The purpose of this research was develop and evaluate a platform for controlled drug deliver systems based on SLN (solid lipid nanoparticle) and a insoluble non-swelable excipient for direct compression (dicalcium phosphate dihydrate (Di-TabTM). SNL were manufactured using glyceryl behenato (Compritol (R)888) by a high shear process in hot.

Mr. Huisuk Yang has graduated both department of mechanical engineering and that of biotechnology from Yonsei university. Since then he is researching in the nanobiotechnology laboratory in Yonsei university as a graduate student for his Ph.D. He has recieved “Best technology transfer and industrialization award” and “Best trial product award” because of his achievements in biotechology field.

Lipophilic drugs have been considered as potential candidates among drug development history. However, due to the need for hazardous organic solvents for their solubilization, these drugs often fail to reach the pharmaceutical market, and in doing so highlight the importance of solvent free systems. Although transdermal drug delivery systems (TDDSs) are considered prospective safe drug delivery routes, a system involving lipophilic drugs in solvent free or powder form has not yet been described. Here, we report, for the first time, a novel approach for the delivery of every kind of lipophilic drug in powder form based on an smart polymeric system (SPS). The phase transition of powder form of lipophilic drugs due to interior chemical bonds between drugs and biodegradable polymers and formation of nano-sized colloidal structures allowed the fabrication of dissolving microneedles (DMNs) to generate a powerful TDDS. We showed that SPS based DMN with powder capsaicin enhances the therapeutic effect for treatment of the rheumatic arthritis in a DBA/1 mouse model compared to a solvent-based system, indicating the promising potential of this new solvent-free platform for lipophilic drug delivery.

Wang Xin is currently a final-year PhD student at National University of Singapore. She has attended several local & international conferences and achieved multiple awards. She has published 1 first-author paper in reputed journal ACS-nano.

Liver cancers are among the most common cancers worldwide and hepatocellular carcinomas (HCCs) account for 75% of all primary liver cancers. In HCCs, potential cancer stem cells (CSCs) have been identified through the isolation of side population (SP) cells according to the ability to efflux Hoechst 33343 dye. These SP cells share many functional properties of CSCs such as extensive self-renewal and proliferative capacity, and more importantly, the ability to initiate tumor growth in immuno-compromised mice. SP cells are also resistant to conventional chemotherapies and are the likely candidates for tumor recurrence owing to the ability to efflux drugs effectively via expression of various ABC drug transporters. Here, we proposed the use of a nanoparticle drug delivery platform, nanodiamonds (NDs) for targeting of these chemoresistant cells. Using ND adsorbed with a common chemotherapeutic agent, Epirubicin (Epi), we demonstrated that these EPND complex can prolong drug retention in tumor cells. More importantly, we also showed that EPND complex can significantly reduced the SP cells as compared to Epirubicin drug alone. Finally, EPND showed significant lower toxicity than Epi. Collectively, ND-conjugated chemotherapy presents a promising avenue for overcoming chemoresistance and tumor recurrence in cancers such as HCC.

Gamal Zayed currently a faculty at Al-Azhar University and published more than 10 articles in international Journals.

The aim of this work was to study the potential of delivering lornoxicam as an efficient potent analgesic drug into a more absorbed, small polymeric sustained release microspheres. The emulsification and solvent evaporation method are most successful methods for drugs that are insoluble in the aqueous medium. Otherwise, the drug will favorably partition into the aqueous phase resulting in low core loading. Lornoxicam was dissolved into ethyl cellulose in methylene chloride. For emulsification using tween 80 and carboxy-methylcellulose as emulsifiers. The emulsion was stirred using Homogenizer Branson 450 for 30 minutes in order to reduce the particles size. Encapsulation efficiency EE%, size and weight of Microspheres loaded with Lornoxicam were determined. Furthermore, the release profiles of Lornoxicam from ethyl cellulose Microspheres were measured in phosphate buffer pH 7.4, as it’s the media required for releasing of ethyl cellulose. The results showed that EE% for all forms of microspheres were decreased with the decrease in drug: polymer ratios. SEM showed synthesized NPs in different shapes such as cubes, rods, and triangles for the LOR coated with glycerin as nanoparticles. Moreover, higher EE% was observed within the GNPs reaching about 83%. The Microspheres had a mean diameter of 50±5µm. The release rate of lornoxicam from Microspheres was strikingly higher than that from drug itself, confirming that the release was enhanced with controlling for the release. The here presented microspheres formulations serve as promising platform to improve the solubility, absorption and sustained release of lornoxicam.

Dr Aldawsari is an Associate Professor of Pharmaceutics. She has completed her PhD from University of Strathclyde, Glasgow, UK at 2011. She is currently the Vice-Dean of Faculty of Pharmacy at King Abdulaziz University in Jeddah, Saudi Arabia. Dr Aldawsari’s research is focused on the development of therapeutic nanoparticle technologies, drug & gene delivery and Biotechnology. She has authored 19 papers in related peer review journals, and has more than 12 funded research projects either as PI or Co-I.

Lemongrass oil is a volatile oil extracted from the leaves of Cymbopogon citratus that has various pharmacologic and clinical effects. The oil suffers from low aqueous solubility and instability of its major active constituent, citral. These drawbacks could lead to reduced effect, volatilization, and consequently, skin irritation. To overcome these problems, this research aims at enhancing the antinfungal activity and reducing irritation of lemon grass via the formulation of topical hydrogel loaded with ethyl cellulose-based nanosponges containing lemongrass. The minimal inhibitory concentration and minimal fungicidal concentration of LGO against Candida albicans strain ATC 100231, determined using the broth macrodilution method, were found to be 2 and 8 µL/mL, respectively. Nanosponges were prepared using the emulsion solvent evaporation technique. The nanosponge dispersions were then incorporated into 0.4% carbopol hydrogels. Nine formulations were prepared according to a 32 full factorial design. Ethyl cellulose: polyvinyl alcohol ratio and stirring rate were studied as independent variables. The prepared formulations were characterized for particle size, citral content, and in vitro release. Results revealed that all the nanosponge dispersions were in the nano range, with satisfactory citral content and sustained release profiles. Both independent variables have significant effects on particle size and percentage released after 6 hours; however, the effect of the stirring rate was more prominent on both responses. Morphological investigations for the selected hydrogel formulation, F9, revealed that the nanosponges possess a spherical uniform shape with a spongy structure that preserved their integrity after incorporation into the hydrogel. Furthermore, the in vivo evaluation proved the non-irritancy and the effective antifungal activity of the selected formulation against C. albicans.

Maulikkumar Patel has completed his PhD at the age of 29 years from Jodhur National University. He is Assistant Professor at Shri B. M. Shah College of Pharmaceutical Education and Research from last eight years. He has published more than 18 national and international papers in reputed journals.

The aim of present investigation was to develop orodispersible film of levocetrizine for increasing bioavailability and patient acceptance. It was prepared by solvent casting method by different polymer and plasticizer. The taste masking was carried out by Drug Resin complex using Kyron T 134 with 1: 3 ratio with drug. A 32 factorial design was applied for optimization.. Prepared film were evaluated for their drug content uniformity, Thickness, Folding endurance, Tensile strength, Percentage elongation, Disintegration time, In vitro drug release and Stability study. The drug resin complex with Kyron T 134 show good taste masking with ratio 3:1. The formulation F5 shows higher drug content 96.54 ± 1.59 %, Less disintegration time 32 ± 1 sec, Tensile strength and folding endurance respectively 0.237 ± 0.067 N/nm2 and 120 ± 3. Film of batch F5 was release 94.3% within 20 min during the in vitro dissolution test.These studies indicate that development of orodispersible film with view to patient compliance and to obtain faster onset of action. According to 32 full factorial designs, F5 proved as an optimized batch. Batch F5 remain stable after 1 month accelerated stability study. Drug excipients are compatible to each other was confirmed by FTIR study.

Ms. Ramasatyaveni is pursuing her PhD from CSIR-Indian Institute of Chemical Technology as a student of Academy of Scientific and Innovative Research (AcSIR), New Delhi. She has published 4 papers in reputed journals including Biomaterials and has presented her research work in several leading research conferences.

Chronic wound remains as a constant challenge for patients with diabetes. Among the present strategies to overcome the failures of wound healing, stem cell transplantation has shown a promising role. However, this technique still suffers from limitations such as high levels of ROS at wound site along with low bioavailability upon systemic administration. To overcome these limitations, we developed a biocompatible and porous scaffold for cell delivery. Utilizing simple urethane chemistry and semi-interpenetrating polymer network approach a polyethylene glycol-polyurethane porous polymer network was generated. The key physico-chemical properties of these polymers were characterized using FT-IR, Raman, SEM, DSC, TG-DTA. The biocompatibility tested on various cell lines as well as mouse primary bone marrow stem (BMSCs) cells isolated from C57BL/6J mice depicted these polymer networks to be highly cytocompatible. The cells cultured in presence of polymer network have shown a ≥6 –fold increase in gene expression of gelatinase and collagenase via activation of Akt and Erk elucidating the mechanism of cellular penetration. Interestingly, H2O2-induced apoptosis of BMSCs was abrogated in presence of polymer networks indicating a protective effect from oxidative stress. Transplantation of BMSC+PEG-PU at murine excisional splint wound site depicted significant increase in fibroblast proliferation, collagen deposition, and anti-oxidant enzyme activities with concurrent reduction in inflammation at the injury site. Finally, immunostaining revealed an enhanced engraftment (stem cell markers expression) and vascularity (CD31) indicating an accelerated wound tissue closure. This pre-clinical study demonstrates the proof-of-concept and further necessitates their evaluation as potential cell delivery vehicle scaffolds in clinical settings.

Kulwinder Kaur has completed her M.Sc.in Applied Physics(Electronics) from Department of Applied Physics, Guru Nanak Dev University, Amritsar. Currently, She is puesuing her Reserach work as DST-INSPIRE Senior Reserch Fellow under the supervision of Prof. K.J.Singh at Department of Physics, Guru Nanak Dev University, Amritsar. Her area of reasech interest is the study the structural and biocompatible behaviour of bio cermaics and bioscaffolds.

Copper doped hydroxylapatite nanoparticles have been prepared by co-precipitation method. Bioscaffolds synthesized from polymers and hydroxylapatite nanoparticles provide necessary sites for bone tissue regeneration. In the presented work, bioscaffolds have been prepared from 1, 6-diisocyanatohexane-extended poly (1, 4-butylene succinate) by solvent casting method from 10% w/v in pure chloroform with 2 wt% of hydroxylapatite nanoparticles containing different amount of copper at room temperature. Prepared scaffolds have been characterized by X-Ray Diffraction, Fourier Transform Infra –Red Spectroscopy, Transmission Electron Microscopy and Field Emission Scanning Electron Microscopy techniques. Incorporation of hydroxylapatite nanoparticles into the polymer matrix has been confirmed from the above mentioned techniques. Potential for use of scaffolds as successful drug delivery system has been checked with gentamycin. Controlled degradation of bioscaffolds is an important parameter. It has been seen that with the increase in the content of hydroxylapatite nanoparticles, degradation increase with leaching of more ions from the scaffold. Effect of pH on biodegradability has been investigated in phosphate buffer saline with two pH values (7.4 and 4.5) in detail. Potential for use of scaffolds as successful implant materials in human body has been checked during in vitro analysis by employing MG-63 cell lines. Results indicate that our scaffolds have the ability to support the cell attachment.

Vikas Anand has completed his M.Sc. in Physics from Jiwa ji University, Gwalior , India . Presently, He is persuing Ph.D. degree in the research area of biomaterials from Department of Physics, Guru Nanak Dev University , Amritsar, India . His area of intertrest is to study the structural and bioactive properties of bioactive glasses and ceramics.

Magnetically attracted silver coated xFe2O4 (x= Mn , Zn ) doped hydroxylapatite samples have been prepared by using co-precipitation method in the laboratory. Bioactive nature of samples has been confirmed from XRD pattrens. Ferromagnetic behavior of samples has been studied by using vibration sample magnetometer technique. Cytotoxicity, antioxidant and cell culture studies of the samples have been undertaken by using human osteoblast cell line MG63 and it was found that samples provides healthy environment for the growth of cell lines. Drug carrier ability of samples has been checked by using gentamycin as an antibiotic and results show that samples can be used as excellent drug carriers. Drug loaded samples can be easily targeted to specific area due to their attractive nature towards external magnetic field. Samples have also shown good resistive potential against different gram positive and gram negative microorganisms including highly resistive Methicillin-resistant Staphylococcus aureus. Our results indicate that prepared samples possess good bioactive as well as ferromagnetic behavior with drug carrier ability and hence , our samples can be potential candidates for the clinical applications.

Luiz Eduardo Nunes Ferreira has degree in Biology sciences and PhD in Pharmacology completed in 2014 at the University of Campinas. Currently, works in postdoctoral studies at the same institution. He has published 8 papers in reputed journals. The main research topics involves studies with local anesthetics associated with modified drug delivery systems and the effects in vitro on cell toxicity and in vivo on models of cancer and pain.

Lidocaine has shown antiproliferative, cytotoxic, apoptotic and anti-inflammatory effects. Therefore, it is a promising drug for the study of antitumor activity. Lidocaine use is restrict due to its short duration of action, however lidocaine biopharmaceutical properties may be improved when it complexes with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD). This study evaluated the in vitro and in vivo effects of HP-β-CD/lidocaine on cell viability, proliferation and tumor growth. Human keratinocytes were exposed in vitro to concentrations ranging from 11.5 – 1,115 µg/mL of lidocaine or HP-β-CD/lidocaine, and cell viability and antiproliferative tests were performed. Walker 256 cells were inoculated in the plantar region of the right paw of Wistar rats. A 0.2 mL solution of 5% lidocaine or 5% HP-β-CD/lidocaine was injected into the intraplantar region. Changes in paw edema were measured daily and the mass of the rat paws were weighed after the end of the experiment. Lidocaine and HP-β-CD/lidocaine at 630 µg/mL significantly reduced cell viability by 70% (± 20.3) and 60% (± 16.7) respectively. The IC50 was approximately 1,115 µg/mL for both formulations. However, plain lidocaine had a stronger antiproliferative effect after 48 hours. In vivo, the control group showed an increase of 3.52-fold in the paw edema on the last day. Treatment with lidocaine and HP-β-CD/lidocaine led to an increase of 2.6-fold and 2.2-fold, respectively, which differed significantly from the control. The mass of the paws also showed difference between the control group (mean 4.28 g) as compared to lidocaine (mean 2.49 g) and HP-β-CD/lidocaine (2.30 g).

Worked at Medipharm Industries EA Ltd.Uganda. factory for 15 yrs. Specialized IN cGMP and ORS Manufacture Studied at Mulago Hospital School of Dispensing for a Dip Pharm 1988 Taught at Mulago Paramedical school for 2 yrs. Attended a Clinical instructors course at Mbale Health Manpower Development Center 1999 Worked as an asst. Drugs Inspector at Uganda National Drug Authority for 7 yrs. Attended At NIPER Chandigarh India Assessment of quality of Pharmaceuticals. Studied at NMMU Port Elizabeth S.Africa for my B. Pharm 2012. Worked at Johannesburg General Hospital Charlotte Maxeke for my Pharmacist Internship.2013 Now M.Pharm Student at the University of the Witwatersrand SA 2013 to 2015.

Back ground and the purpose of study: At present, pharmaceutical researchers are focusing on instantaneous intraoral dispersible technologies as novel drug delivery systems because of their outstanding advantages over the traditional oral and parenteral routes of drug administration. Most essential natural drugs have low oral bioavailability due to extensive first pass metabolism and pre systemic degradation in the GIT. This research intends to addresses these problems by formulating a cheap, intraoral rice paper Intraoral Dispersible Film (IDF). IDFs are potent and could improve bioavailability of natural drugs. Methods: In this study, formulation was optimized using the experimental factorial design. The IDFs were loaded with model natural anticancer drugs Resveratrol and Curcumin with low oral bioavailability. They were evaluated for thickness, folding endurance, swelling behavour because these relate to drug release properties. Permeation was also evaluated using the pig mucosal membrane mounted on a Franz diffusion cell, and taste testing was done to determine acceptability using a taste panel. Results: Sixteen formulations showed variations in disintegration time, thickness, Tensile strength and permeation profiles. My key finding is, ex vivo release profiles of the optimized formulation revealed first order release and later zero order. Conclusions: Therefore, it is evident that rice paper IDF could efficiently deliver natural drugs into the blood.