FORMULATION STRATEGIES FOR GASTRORETENTIVE DELIVERY OF ATAZANAVIR: IN VITRO EVALUATION AND OPTIMIZATION

Abstract

The present study aims to develop and evaluate gastroretentive floating tablets of Atazanavir sulfate to prolong gastric residence time and enhance oral bioavailability. Atazanavir, a BCS class II drug, exhibits pH-dependent solubility and limited absorption in the upper gastrointestinal tract. Floating drug delivery systems can offer sustained release and enhanced bioavailability by remaining buoyant in the gastric environment. Tablets were formulated using polymers such as Ethyl cellulose, and Sodium alginate in various concentrations. Sodium bicarbonate was incorporated as a gasgenerating agent. The tablets were evaluated for pre-compression and post-compression parameters, including hardness, friability, floating lag time, total floating time, drug content, and in vitro drug release. The optimized formulation F3 showed a floating lag time of 47 seconds and total floating time exceeding 12 hours, with sustained drug release of over 93.35% at the end of 8 hours. The results support the use of floating matrix tablets as a potential gastroretentive strategy for improving Atazanavir sulfate therapy.