Preparation, characterization and in vitro evaluation of cisplatin-bound triblock polymeric micelle solution for ovarian cancer treatment.

The main objective of this study was to prepare cisplatin (CDDP) bound triblock polymeric micelle solution which will have a 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 the 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 the 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.

The novel oral imatinib microemulsions: physical properties, cytotoxicity activities and improved Caco-2 cell permeability.

The objective of this study was to formulate imatinib (IM) loaded to water-in-oil (w/o) microemulsions as an alternative formulation for cancer therapy and to evaluate the cytotoxic effect of microemulsions Caco-2 and MCF-7. Moreover, permeability studies were also performed with Caco-2 cells. W/o microemulsion systems were developed by using pseudo-ternary phase diagram. According to cytotoxicity studies, all formulations did not exert a cytotoxic effect on Caco-2 cells. Furthermore, all formulations had a significant cytotoxic effect on MCF-7 cells and the cytotoxic effect of M3IM was significantly more than that of other microemulsions and IM solution (p < 0.05). The permeability studies of IM across Caco-2 cells showed that permeability value from apical to basolateral was higher than permeability value of other formulations. In conclusion, the microemulsion formulations as a drug carrier, especially M3IM formulation, may be used as an effective alternative breast cancer therapy for oral delivery of IM.