In-vitro and in-vivo evaluation of novel injectable contraceptive preparations of Centchroman

Objectives: The in vitro release profile, stability and anti-fertility efficacy of some injectable, biodegradable formulations of Centchroman was investigated. Methods: The formulations included an in situ gelling preparation namely Poly(Lactide-co-Glycolide) (PLGA)-in-Triacetin prepared by solution method and Niosomes prepared by lipid layer hydration method. These were evaluated for physicochemical characteristics like size distribution, percentage entrapment, in vitro drug release profiles in phosphate buffered saline (pH 7.4) and stability at different conditions of storage viz; 4°C, room temperature and 37°C. In vivo anti-fertility activity was evaluated in female albino rats showing normal oestrous cycle by giving a single dose of the formulation (5mg/kg body weight) and then checking for number of implantations on 20th day of pregnancy. Also histopathological sections of the uterus and ovary were studied for further evaluation. Results: The formulations showed controlled drug release and enhanced stability whereas in vivo studies showed promising anti-fertility activity for PLGA-in-Triacetin. Conclusions: It was evident from this study, that, PLGA-in-Triacetin was a better candidate for development of a biodegradable, bio-erodable, long acting, injectable contraceptive formulation.