Irfan Akartas

The main purpose of this study is to design Cefpodoxime proxetil (CFP) loaded Eudragit RS 100 (ERS) nanoparticles to provide prolonged drug release, the enhanced oral efficacy of the drug at a lower oral dose. CFP-loaded nanoparticles are prepared by the single-emulsion solvent evaporation method with different drug:polymer ratios, F1 (CFP:ERS=1:1) and F2 (CFP:ERS=1:2). Physicochemical characterization, antibacterial activity, cytotoxicity profiles of nanoparticles are examined. F1 and F2 nanoparticles have a particle size of 236.70±3.05 and 258.87±11.32 nm, spherical shape, and a porous surface under SEM. The zeta potential values of F1 and F2 nanoparticles were 22.13±1.01 and 25.80±2.01 mV, and the encapsulation efficiencies were 34.37±3.71% and 55.78±3.52%, respectively. Since F2 nanoparticles have a smaller particle size, higher zeta potential, and encapsulation efficiency, this formulation was chosen as superior, and the subsequent experiments were continued with this formulation. The antibacterial activity of F2 nanoparticles against E.coli was found to be 2 times more effective than CFP. Cytotoxicity studies revealed that the cell viabilities in BEAS-2B and HepG2 cells were higher with the exposure to CFP nanoparticles (200 µg/ml) compared to CFP (100 µg/ml) alone. CFP nanoparticles have excellent efficacy and a cytocompatible profile in inhibiting the growth of bacteria compared to free CFP.

The main objective of this study was to prepare cisplatin (CDDP) bound triblock polymeric micelle solution which will have hydrophilic shell not being phagocytosed by mononuclear phagocyte system, and evaluate in vitro behavior for the treatment of ovarian cancer. For this aim, CDDP was bound to polyglutamic acid (PGA) and triblock polymer was prepared using polyethylene glycol)-polylactide-co-glycolide (PEG-PLGA). CDDP-bound triblock copolymer conjugation was characterized, in vitro release and permeability studies were performed using USP II method and CaCo-2 cell lines respectively. The release of CDDP from CDDP-bound triblock polymeric micelle solution was found 87.3 ± 3.56% at the end of 24th hour. CDDP bound triblock polymeric micelle solution was detected as biocompatible, and permeable according to in vitro studies. According to the MTT results, the measured cytotoxicity was found to be maximum in CDDP-bound triblock polymeric micelle solution when compared with CDDP solution and conjugate in SKOV-3 and OVCAR-3 cells whereas Annexin V-FITC Apoptosis results were found to be maximum in A2780 cells.