Abstract

PROGESTERONE BEARING MICROEMULSION GEL AUGMENTED DRUG PERMEATION THROUGH INTRAVAGINAL ROUTE OF ADMINISTRATION: IN VITRO AND IN VIVO STUDY

Shekhar Sharma*, Anupama Diwan, Rupali Kalra and Vandana Arora

ABSTRACT

There is a need for novel formulations to improve the bioavailability through the vaginal/rectal mucosa of progesterone for contraception. Here we have presented recent discovery of novel gel-microemulsions (GM) as nontoxic, dual-function intravaginal contraceptive which can be used as delivery vehicles for lipophilic drug substance. We describe the formulation and permeation of progesterone bearing microemsulion gel with drug loading capacity of 346.78±11.35 mg/ml. The tailored microemuslion gel of progesterone comprising oil-in-water microemulsion and polymeric hydrogels were designed to solubilize the progesterone and exhibited rapid permeation across vaginal mucosa. Preclinical studies comparing the in vivo permeation efficacy of progesterone bearing microemuslion gel versus marketed cream. The optimized progesterone microemulsion vaginal gel displayed superior permeation (225 μg/ml) across the vaginal barrier as compared to marketed vaginal progesterone gel (45 μg/ml). Unlike the marketed cream of progesterone, intravaginal applications of progesterone bearing microemuslion gel in the rat vagina did not show any inflammation or damage of the vaginal mucosa or epithelium. Furthermore, in short, it was not associated with any local, systemic, or reproductive toxicity. Hence, progesterone bearing microemuslion gel displayed superior efficacy as compared to marketed cream.

Keywords: Progesterone, microemulsion gel, vaginal route of administration, drug permeation.