Formulation, Development and Evaluation of Anti-Implantation Activity of Intrauterine System of Centchroman (Saheli) using Wistar Albino Rats

Abstract

Centchroman – A Non-steroidal, post-coital anti-implantation drug which is generally popular as SAHELI is one of the best agents available. The fundamental aim of this study  was to formulate such an Intra-uterine System of Centchroman which should be safe and acceptable. This new drug delivery system surpasses the first pass metabolism, thus increasing the bioavailability and reducing the drug load. This formulation delivered the drug upto 21 days. Polylactic-co-glycolic acid served as the best fit polymer for delivering the drug. The best optimized formulation was selected and subjected to stability studies. The effect of the foreign bodies was also observed on the fertility, mating behaviour and estrous cycle of the rats along with anti-implantation activity of the IUS. This formulation was tested on Wistar albino rats and is proved to be safe at the optimized dose level. The formulation exhibited pre-implantation loss of 100% and post-implantation loss of 0% in Wistar albino rats at a particular dose when delivered on 1^stday and 4^th day post-coital. Experimental part on animals showed that any foreign body, if put inside the uterus would not affect the fertility unless the size is more than 6mm. Results showed that 3mm objects had no effect on fertility. The foreign bodies and the IUS showed neither any alteration in the estrous cycle nor on the mating behavior of the animals.