Abstract

ENHANCEMENT OF GASTRIC RESIDENCE TIME OF ATAZANAVIR VIA FLOATING DRUG DELIVERY SYSTEM

*Dr. A. Sambasivarao M.S Ph.D, E. Venkata Sai, G. Lakshman, Mathe Ark

ABSTRACT

Enhancement of Gastric Residence Time of Atazanavir via Floating Drug Delivery System Atazanavir sulphate (ATV) is a potent HIV-1 protease inhibitor widely used in the treatment of Human Immunodeficiency Virus (HIV) infection. However, its oral bioavailability is limited due to pH-dependent solubility, reduced absorption in the intestinal environment, and a relatively short biological half-life of approximately 5–7 hours. The present study was undertaken to develop and evaluate gastroretentive floating mini-tablets of Atazanavir sulphate to prolong gastric residence time, enhance drug absorption, and provide sustained drug release. Floating mini-tablets were prepared using various low-density polymers, including ethyl cellulose, carbopol, guar gum, and polypropylene foampowder, by direct compression technique. Both effervescent and non-effervescent formulations were developed and filled into hard gelatin capsules. The prepared formulations were evaluated for pre-compression and post-compression parameters, buoyancy characteristics, swelling behavior, drug content, and in-vitro dissolution performance. The formulated mini-tablets exhibited satisfactory flow properties, acceptable physical characteristics, and prolonged buoyancy in simulated gastric fluid. In-vitro dissolution studies demonstrated sustained drug release over an extended period, with the release profile significantly influenced by the type and concentration of polymer employed. Drug release kinetics were analyzed using Zero-order, First-order, Higuchi, and Korsmeyer–Peppas models to elucidate the mechanism of release. The results indicate that gastroretentive floating mini-tablets of Atazanavir sulphate can successfully enhance gastric retention and sustain drug release, thereby offering a promising approach to improve oral bioavailability and reduce dosing frequency. The developed floating drug delivery system may contribute to improved therapeutic efficacy and patient compliance in antiretroviral therapy.

Keywords: Atazanavir sulphate, Gastroretentive drug delivery system, Floating mini-tablets, Sustained release, Gastric residence time, Bioavailability, HIV therapy.