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

• Published in: Drug development and industrial pharmacy Vol. 47; no. 8; pp. 1248 - 1260
• Main Authors: Ak, Güliz, Akartas, Irfan, Özel, Buket, Selvi Günel, Nur, Karasulu, Hatice Yeşim, Gümüştaş, Barış, Karasulu, Ercüment, Hamarat Şanlıer, Şenay
• Format: Journal Article
• Language: English
• Published: England Taylor & Francis 03.08.2021
• Subjects: A2780; Cisplatin; ovarian cancer; OVCAR-3; polymeric micelle; SKOV-3; polymeric micelle; OVCAR-3; A2780; ovarian cancer; SKOV-3; Cisplatin
• ISSN: 0363-9045; 1520-5762
• DOI: 10.1080/03639045.2021.1989451

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.