Abstract

DEVELOPMENT AND EVALUATION OF A SUSTAINED RELEASE GASTRORETENTIVE DOSAGE FORM OF ATENOLOL IN THE FORM OF FLOATING MICROSPHERES

Shivani Kundap*, Seema Jadhav, Manisha Karpe and V. Kadam

ABSTRACT

Atenolol floating microspheres were prepared by non-aqueous emulsion solvent evaporation method with polymer ethyl cellulose to increase the gastro retention time. Attempts were made to enhance the bioavailability, to increase the gastric residence of the drug, to provide a site specific controlled release and to restrain and localize the dosage form in the stomach thus prolonging the gastro retention time of drug. Various batches were taken, out of which Atenolol optimized batch 7 (ATO-7OP) was finalized and formulated with polymer ethyl cellulose and the mixture of ethanol and dichloromethane as the solvent system for further evaluation and stability studies. The flow properties were assessed using metrics like angle of repose, compressibility index, as well as other physicochemical features like particle size, percent entrapment efficiency, percent buoyancy, and in vitro drug release. Batches with single ethyl cellulose polymer and different drug to ethyl cellulose ratios gave good results for floating microspheres. Stirring speed of 800 rpm and drug to polymer ratio of 1:13 was found to be optimum. Scanning electron microscopy showed hollow cavity with porous nature of the microspheres. Ethyl cellulose polymer sustained the drug release for about 24h. Drug release kinetics best fitted in First order followed by Higuchi drug release concentration dependent and microspheres followed diffusion controlled release mechanism. The developed atenolol floating microspheres exhibited prolonged drug release in simulated gastric fluid for 24 h, and, therefore, could potentially improve the bioavailability of the drug as well as patient compliance.

Keywords: Atenolol, Floating Microspheres, Adrenergic Beta-1 Receptor Antagonists, Cardiovascular diseases.