14^th International Conference and Exhibition on Pharmaceutical Formulations August 28-29, 2017 Brussels, Belgium

Tomasz Urbaniak is a Pharmacist and Research Assistant in Physical Chemistry Department of Faculty of Pharmacy, Wroclaw Medical University. His activity includes evaluation of polymerization methods, structural analysis of polymeric materials on molecular and bulk level, and examination of drug release from nanometric and micrometric particles. Also, utilization of quantum chemistry calculations in the field of pharmaceutical science is in scope of his interests. Interdisciplinary approach is the way he thinks and acts in his work.

Poly-E-caprolactone (PCL) is biodegradable, nontoxic polyester synthesized mainly in ring-opening polymerization (ROP) of E-caprolactone (CL). PCL alone or in blends was utilized in numerous medical applications, such as scaffolds, implants, nano- and micro- drug carriers. It is characterized by slow degradation of polyester chains in hydrolytic mechanism. Lamivudine (LV), as well as other antiretroviral drugs used in HIV-1 treatment, targets infected immune system cells, mainly CD4+ T helper cells. However, other infected cells like macrophages, monocytes, dendritic cells are found through whole body, including lungs and central nervous system. This cells halflife, measured in weeks/years, is dramatically longer in comparison to CD4+ T helper cells, which is counted in hours/days. Such cells are often recognized as reservoirs of retroviruses, especially these which are found in sites hardly available for drug substances, so called “sanctuaries”. The aim of this study was to design a process of poly-E-caprolactone-lamivudine conjugate (PCL-LV) synthesis, and forming it into microspheres. Due to extremely slow hydrolytic degradation, phagocytosis would be main mechanism of intravenously administered particles clearance. Suggested mechanism of ROP includes formation of bond between initiator and polymer backbone. Drug bound covalently to oligomeric chain would not be released from polymeric matrix in to plasma, therefore whole administered dose would eventually achieve phagocytic cells, i.e., HIV-1 infected macrophages, monocytes or dendritics cells. Conjugate structure was confirmed by the proton nuclear magnetic resonance and electro-spray ionization time of flight mass spectroscopy. Further stage of study included microsphere forming in a variant of solvent evaporation method. Shape and size of obtained particles was determined by scanning electron microscopy, light microscopy and dynamic light scattering. Average molecular weight of obtained polymers was 5400 Da, size of prepared particles varied from nanometric to micrometric dimensions. Recent Publications 1. Woodruff MA, Hutmacher DW (2010) The return of a forgotten polymer—polycaprolactone in the 21st century. Prog. Polym. Sci. 35:1217–1256. 2.Orozco-Castellanos LM, Marcos-Fernández A, Martínez-Richa A (2011) Hydrolytic degradation of poly(ε-caprolactone) with different end groups and poly (ε-caprolactone-co-γ-butyrolactone): characterization and kinetics of hydrocortisone delivery. Polym. Adv. Technol. 22:430–436. 3. Koppensteiner H, Brack-Werner R, Schindler M (2012) Macrophages and their relevance in Human Immunodeficiency Virus Type I infection. Retrovirology 9:82. 4. Alexis F, Pridgen E, Molnar LK, Farokhzad OC (2008) Factors affecting the clearance and biodistribution of polymeric nanoparticles. Mol. Pharm. 5:505–515. 5. Storey RF, Sherman JW (2002) Kinetics and mechanism of the stannous octoate-catalyzed bulk polymerization of ε caprolactone. Macromolecules 35:1504–1512.

Supamas Napavichayanun is a PhD student, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Thailand. She earned a BSc from Faculty of Pharmaceutical Sciences, Chulalongkorn University in 2010. Her research experience has ranged from protein including silk proteins and biomaterials. She also did clinical researches in the area of dermatology especially materials for wound healing application.

Sericin has been conducted to characterize its immunomodulatory effects especially anti pro-inflammatory activities for decades.In addition, it is also well known that hyperpigmentation disorders such as post inflammatory hyperpigmentation (PIH) and melanoma, are a major concern not only in white skin type people, but also raises in darker skin type of Asian population. Although there are many types of therapeutic products, more effective treatments still need to be evolved. The important modulators of epidermal innate immune responses are melanocytes and dendritic cells (DCs), which composed of induction, regulation, and maintenance of inflammatory responses on skin. However,the immunomodulatic role of sericin on melanocytes and DCs relate to therapeutic effect of hyperpigmentation disorders has not been well established. Moreover,sericin composes of the anti-tyrosinase property. Although the most prominent target for inhibitors of hyperpigmentation is tyrosinase, unfortunately, a little is known about its anti-melanogenic property and clinical efficacy. In this study,we conducted in vitro model and electron microscopic studies (immune-gold labeling) to determine (i) the tolerogenic effect sericin on melanocytes and DCs indicated by the level of IL-10 and transforming growth factor (TGF)-ß, (ii) the anti-melanogenic property of sericin characterized by tumor progressive marker (Mtif) and (iii) the anti-tyrosinase effect of sericin using tyroninase marker. The results showed that sericin (at leat 5 μg/ml) composed of tolerogenicity, anti-tyroninase and anti-melanogenicity effects on melanocytes and DCs as demonstrated by the up-regulation of IL-10 and TGF- ß in association with the down-regulation of tyrosinase and Mtif, respectively. This study provides the understanding of immunomodulatic role of silk sericin on melanocytes and DCs underlying hyperpigmentation disorders lead to the applications allowing affected people to have a better quality of life and their guidelines for therapeutic approaches. Recent Publications 1.Napavichayanun S, Amornsudthiwat P, Pienpinijtham P, Aramwit P (2015) Interaction and effectiveness of antimicrobials along with healing-promoting agents in a novel biocellulose wound dressing. Materials Science and Engineering C 55: 95-104. 2.Napavichayanun S, Yamdech R, Aramwit P (2016) The safety and efficacy of bacterial nanocellulose wound dressing incorporating sericin and polyhexamethylenebiguanide: In vitro, in vivo and clinical studies. Archives of Dermatological Research 308: 123-132. 3.Napavichayanun S, Aramwit P (2017) Effect of animal products and extracts on wound healing promotion in topical applications: a review. Journal of Biomaterials Science, Polymer Edition. 28(8):703-729. 4.Ampawong S, Isarangkul D, Aramwit P (2017) Sericin ameliorated dysmorphic mitochondria in high-cholesterol diet/streptozotocin rat by antioxidative property. Experimental Biology and Medicine 31(9): 1011-1021. 5.Aramwit P, Motta A, Kundu SC (2017) Tissue engineering: from basic sciences to clinical perspectives. Biomed Research International 2017:8659036. doi: 10.1155/2017/8659036.

Kampanart Huanbutta has his expertise in drug delivery system and application of polymer in pharmaceutical dosage forms. He graduated from Faculty of Pharmacy, Silpakorn University, Thailand. After that, he received Postdoctoral Scholarship from Erasmus Mundus to conduct research concerning anticancer drug delivery system in University of Porto, Portugal. Now he is working at Faculty of Pharmaceutical Sciences, Burapha University as an Assistant Dean for academic affair and post-graduation study. He also works as Secretary General of Pharmaceutical Association of Thailand under Royal Patronage. He has published research and review articles in international journals for more than 20 articles.

Crude seed gum and their carboxymethyl derivatives from Cassia fistula seed was developed and characterized to apply as the pharmaceutical disintegrant in fast disintegrating Thai cordial tablet. The chemical structure of crude gum was chemically modified via carboxymethylation. Degree of substitution (DS) of carboxymethylated gums was determined. Carboxymethylated gums with minimum and maximum DS values were chosen for further application. IR absorption spectra of gum samples were observed to verify their chemical structure changes. In physical properties, the intrinsic viscosity and swelling property of all gum samples were evaluated. The results showed that carboxymethylated gums had higher intrinsic viscosity than those of crude gum. Moreover, they could swell and be soluble in cold water better than those of crude gums. In conclusion, the modified gums from both plants could provide higher hardness and be better used than that crude gums for fast disintegrating Thai cordial tablet. However, this is a preliminary assessment to expressing pharmaceutical application possibility of these gums as disintegrants, diluents and drug release controlling agents. Recent Publications 1.Anand N, Singh L, Sharma V (2013) Emergence of natural super-disintegrants in oro-dispersible tablets: An overview. Int Res J of Pharm 4: 33-37. 2.Singh V, Kumar P (2011) Carboxymethyl tamarind gum–silica nanohybrids for effective immobilization of amylase. J Mol Catal B-Enzym 70: 67-73. 3.Srivastava M and V P Kapoor (2005) Seed galactomannans: an overview. Chem Biodivers 2(3): 295-317. 4.Zietsman S et al. (2007) Formulation development and stability studies of aqueous metronidazole benzoate suspensions containing various suspending agents. Drug Dev Ind Pharm 33(2): 191-7. 5.Ahuja M et al. (2013) Mimosa pudica seed mucilage: isolation; characterization and evaluation as tablet disintegrant and binder. International Journal of Biological Macromolecules. 57: 105-110.