16^th International Conference and Exhibition on Pharmaceutical Formulations July 26-27, 2018 Rome, Italy

Vivek Puri has completed his Master’s Degree from Chitkara University. He is currently pursuing PhD from Chitkara College of Pharmacy at the same university. He has been awarded at several national and international conferences as a Best Presenter. He has communicated more than 5 papers in reputed journals and has been serving as an Assitant Professor at Chitkara University in Industrial Teaching at Dr.Reddy’s Laboratory.

Mucoadhesion is the process of binding a material to the mucosal layer of the body. Utilizing both natural and synthetic polymers, mucoadhesive drug delivery is a method of controlled drug release which allows for intimate contact between the polymer and a target tissue. It has the potential to increase bioavailability, decrease potential side effects and offer protection to more sensitive drugs such as proteins and peptide based drugs. Thiolation of jackfruit gum polysaccharide was carried out by esterification with thioglycolic acid. Thiolation was confirmed by Fourier-transformed infrared spectroscopy. Jackfruit–thioglycolic acid conjugate were found to possess 468.08 mM of thiol groups as determined by Ellman’s method respectively. Comparative evaluation of mucoadhesive property of irbesartan loaded buccal pellets of jackfruit gum and thiolated jackfruit gum using chicken buccal pouch membrane revealed higher ex vivo bioadhesion time of thiolated jackfruit gum as compared to jackfruit gum. Improved mucoadhesive property of thiolated jackfruit gum over the jackfruit gum can be attributed to the formation of disulfide bond between mucus and thiolated jackfruit gum. In-vitro release study conducted using 0.1N Hcl buffer revealed a sustained release profile of irbesartan from thiolated jackfruit pellets as compared to jackfruit pellets. In conclusion, thiolation of jackfruit gum improves its mucoadhesive property and sustained the release of irbesartan over a prolonged period.

Ameya Sharma has completed her Masters in Pharmacy from Chitkara College of Pharmacy, Chitkara University, India. She is currently pursuing her Doctorate of Pharmacy at the same university. She has been awarded for her research work in global conferences and national conferences. She has communicated more than 5 papers in reputed journals and has been serving as an Assistant Professor in Industrial Teaching at Dr.Reddy’s Laboratories, Baddi, India.

Wound healing is a complex and dynamic biological process. In recent years, the development of new wound dressing products from marine sources is gaining increased interest due to their unique properties such as antimicrobial activity(e.g. chitosan), its biocompatible, biodegradable, non-toxic and non-allergenic nature. Most of these peculiar properties arise from the presence of primary amines along the chitosan backbone. This study was aimed to formulate a hybrid combination of papaya leaves extract and aloevera for developing antimicrobial activity and wound healing applications. Aqueous leaves extract from papaya and aloevera and their hybrid combination were used to develop chitosan fibers. Chitosan polymer containing these extracts was extruded in calcium chloride bath to develop Aloevera (AV), papaya (PP) and their hybrid combinationbased chitosan fibres AP1-AP5. The wound healing properties of the selected combination will be synergistic with the selected natural extract to be incorporated in the all fibers. Molecular mechanistic studies were studied for molecular interaction between the combination of natural extract and and their effect on physicochemical properties of the fibers. The surface morphology, spectra, liquid absorption, tensile strength and anti microbial activity of different batches of the microfibers were evaluated. Aloevera fibers showed greater tensile strength than the papaya extract fibers. The liquid absorption property of all developed fibers decreased, but showed anti-bacterial growth to 70% as compared to pure chitosan fibers. Aloe vera, papaya and hybrid extract-based chitosan microfibers have great potential to be used in wound dressings.

Ayse Nurten Ozdemir has completed her PhD from the Faculty of Pharmacy, Ankara University, Turkey. She has published more than 60 papers in reputed journals and has been serving as the Head of Pharmacuetical Technology Department in same university. She has studied the subjects; solubility enhancement, controlled release dosage forms and has deep concern over implantable systems and floating dosage forms.

The aim of the study is to produce PVA nanofibers, which have attracted considerable interest in recent years due to the high tissue compatibility. Electrospinning was used for the production of nanofibers and the effects of the parameters such as,viscosity, surface tension and electrical conductivity of polymeric solution altered by concentration and surfactant addition are examined.Furthermore the effects of the amount and type of the added surfactants on the properties of polymer solutions and on obtained nanofibers are investigated as well. For the preparation of PVA nanofibers different concentrations of PVA50.000 were dissolved in hot water. After anionic (Sodium dodecyl sulfate), cationic (Benzyldimethyl hexadecylammonium chloride) and nonionic (Polysorbate20) surfactants (0.5-1, 5% w/w) were added, the solutions were poured in a syringe. For electrospinning, the voltage was applied at 20 kv with 0.3 ml/h flow rate and the distance between the needle and the collector was fixed at 15 cm. Viscosity, conductivity and surface tension of the solutions were measured. Nanofiber was characterized by Scanning Electron Microscope (SEM). Ideal concentration of PVA50.000 was found to be 20% w/w for uniform nanofibers. According to the results, when the concentration of anionic and cationic surfactants were increased, the viscosity and conductivity of PVA solution were increased while the surface tension was decreased. It was found that the average diameter of nanofibers was decreased when surfactants, except nonionic forms, were incorporated into PVA solutions. To conclude, it can be stated that anionic and cationic surfactants have multifold effects on the physicochemical properties of the PVA solution whereas nonionic surfactants are not as effective as anionic and cationic forms.

Tamás Jordán holds a MSc Degree in Pharmaceutical Engineering and is currently writing his PhD thesis. He has been working at NanGenex Inc for 5 years,gaining experience in the formulation of poorly water soluble active ingredients. He is interested in the physicochemical background of nanoformulation and bioavailability increasing technologies.

Abiraterone Acetate (AA) is a poorly water soluble drug molecule indicated for patients with metastatic castration resistant prostate cancer. It is a prodrug, which is converted to abiraterone in vivo. The oral dose is high; 1,000 mg which is administered once daily as 4x250 mg Zytiga® tablets. The absolute bioavailability of abiraterone following the administration of Zytiga® is estimated to be below 10% in the fasted state with a 10-fold (AUC) and up to a 17-fold (Cmax) increase following a high-fat meal. We have developed a nano-amorphous AA formulation prepared by controlled precipitation followed by lyophilization. The formulation exhibited higher apparent solubility and passive permeability when compared to either the crystalline AA or Zytiga. In beagle dog studies, this resulted in a >10-fold increase in bioavailability in the fasted state when compared to the marketed drug and the elimination of the food effect. After the preclinical investigation a first-inhuman clinical trial was conducted. Based on the analysis of pharmacokinetic data~250 mg oral dose of the nano-amorphous formulation is expected to result in the same exposure as 1,000 mg Zytiga® in the fasted state. The substantial positive food effect seen for Zytiga® was eliminated. This might allow the reduction of the dose and could eliminate the requirement of taking the drug on an empty stomach. Also, the novel formulation is expected to exhibit smaller variability when compared to Zytiga®.In conclusion we have developed a novel nano-amorphous AA formulation that significantly outperformed the marketed product in in vitro and in vivo tests. Ultimately, the formulation might allow a 75% dose reduction and negate the restriction of a food label.

Žofie Trpělková is in the 2nd year of her Doctoral studies Faculty of Pharmacy in Hradec Králové Charles University, Czech Republic. She pursued her Master studies in Pharmacy (2016) and defended her master thesis in the Department of Pharmaceutical Technology at the same university, Czech Republic, where she studied compressibility of pellets made of microcrystalline cellulose. Recently, she studies the fractal aspects of flow and consolidation behaviour of different excipients including cellets. Her results were presented at the Central European Symposium on Pharmaceutical Technology in Belgrade and at conferences in the Czech Republic and Slovakia.

Microcrystalline cellulose (MCC) is one of the most commonly used excipients in pharmacy, particularly in direct compaction of tablets. Many types of MCC with different particle size and flow properties are produced by pharmaceutical companies. The aim of this work was to characterize flow and consolidation properties of three types of powder microcrystalline cellulose - MCC 101, MCC 102, MCC 200, and Cellets 100, the pellets made of microcrystalline cellulose. All materials were characterized for the moisture content and microscopy characteristics. Flow properties: the bulk, tapped and true density, the angle of repose, and the flow rate through an orifice were evaluated in accordance with Ph. Eur. 9.0. The dynamic of apparent density change under gravity tapping was used to describe the powder bed consolidation behaviour in detail. The results showed that Cellets have significantly higher bulk density and better flow properties than MCC particularly when compared with MCC 101 and 102. The reduction of powder bed volume by gravitational tapping was faster as well. The narrow particle size distribution, the smooth spherical shape and the good flow behaviour of Cellets make them the promissing drug carrier material. In our experience, unfortunately, their compaction properties are poor. The binar or ternar mixtures with MCC will be studied in further to enhance compactability and to reach tablets of acceptable mechanical properties.

Amal Abukhares is currently pursuing her PhD in Pharmacy and Pharmaceutical Sciences at the University of Manchester, England. She has published more than 5 papers in international journals.

Introduction: rhIL-1Ra is a recombinant form of the natural anti-inflammatory mediator, interleukin-1 receptor antagonist that competitively binds with type I receptors (IL-1RI). It inhibits effects of other inflammatory mediator, interleukin -1 (IL-1). However, the rhIL-1Ra has tendency to aggregate at high temperatures and is hence stored at 2°C to 8°C. Aim: The overall project aim is to study thermal stability of the rhIL-1Ra and investigate changes in the secondary structures within the nucleation phase. This may provide clues to reduce the rate of aggregation of protein. Methods: Initially, visual inspection (photographs) was made following the incubation of rhIL-1Ra at 37°C. Then, the aggregation was followed quantitatively by recording changes in the optical density. A more sensitive technique was also used to follow aggregation in the nucleation phase, where sub-visible particles may exist, using particle sizing. The formation of non-native β-structure of the protein was followed by use fluorescence spectroscopy using Thioflavin T (THT). Attempts were also made, using circular dichroism (CD), to assess any induced changes in the secondary structure of the protein induced thermally. Results & Conclusions: Our study suggests that rhIL-1Ra has visible signs of cloudiness within 6 hrs at 37°C. When this is followed by light scattering over 24 hrs period a number of kinetic phases due to aggregation were observed starting with a nucleation phase where changes in particle size were observed. Protein assay indicated a trace amount of rhIL-1Ra was aggregated. Fluorescence assay in particular the Thioflavin T, and CD spectrum results provide earlier indication of formation of non-native beta structures.

Lee Deok-Won is currently working as a Professor at Department of Oral & Maxillofacial Surgery Kyung Hee University Dental Hospital at Gangdong (Kyung Hee Neo Medical Center ) School of Dentistry, Kyung Hee University.

The most ideal implant models in the dental and orthopedic fields to minimize the failure rate of implantation involve the improvement of osseointegration with host bone. Therefore, focus of this study is to prepare surface-modified titanium (Ti) samples of disc and screw types using dexamethasone (DEX) and/or growth and differentiation factor-5 (GDF-5), as well as the evaluation of their efficacies on bone formation in vitro and in vivo. X-ray photoelectron spectroscopy (XPS), scanning electron microscopy (SEM) and contact angle measurement were used to evaluate the surface chemical composition, surface morphology and wettability, respectively. The results showed that implant surfaces were successfully modified with DEX and/ or GDF-5, and had rough surfaces along with hydrophilicity. DEX, GDF-5 or DEX/GDF-5 on the surface-modified samples were rapidly released within one day and released for 28 days in a sustained manner. The proliferation and bone formation of MC3T3-E1 cells cultured on pristine and surface-modified implants in vitro were examined by cell counting kit-8 (CCK-8) assay, as well as the measurements of alkaline phosphatase (ALP) activity and calcium deposition, respectively. MC3T3-E1 cells cultured on DEX/GDF-5–Ti showed noticeable ALP activity and calcium deposition in vitro. Active bone formation and strong osseointegration occurred at the interface between DEX/GDF-5–Ti and host bone, as evaluated by micro computedtomography (micro CT) analysis. Surface modification using DEX/GDF-5 could be a good method for advanced implants for orthopaedic and dental applications.