FABRICATION AND CHARACTERIZATION OF NON STEROIDAL ANTI-INFLAMMATORY ALGINATE BEADS FOR SUSTAINED RELEASE USING NATURAL POLYMER

Abstract

Extended release formulations are becoming more popular day by day for the delivery of non-steroidal anti-inflammatory drugs (NSAIDs) because of their ability to maintain optimal and therapeutically effective drug levels for prolonged duration with the reduction in dosing frequency and side effects associated with NSAIDs. Etodolac is a nonsteroidal anti-inflammatory drug. it is an inhibitor of cycloxygenase which belongs to the pyranocarboxylic acid group, which is effective in treating fever, pain, and inflammation in the body, which is degraded in the stomach. In the present study, a suitable particulate system of Etodolac has been developed, by ionotropic gelation method for sustained release that would result in prolonged clinical efficacy, reduced frequency of administration and lesser side effects. Microbeads were fabricated with and without using guar gum as polymer and were characterized for particle size and size distribution analysis, flow properties, loose surface crystal study, entrapment efficiency, swelling ratio, percentage yield and drug content uniformity and in-vitro drug release. It was found that the particle size distribution of both formulations was varied within a narrow size range. Drug leaching (14.98 % ± 0.118) was more with the presence of guar gum. Entrapment efficiency was retarded with the presence of guar gum. Swelling ratio (53.49 ± 1.874) advocated that guar gum incorporated microbeads swelled more to behave as a matrix for controlled drug delivery. Establishment of highly viscous dispersion with the incorporation of polymer led to high percentage yield (49.35% ± 01.230). Drug release data was fitted to various kinetic models and indicated that the mechanism was according to peppas model. The study discovered that the microbeads of Etodolac could be efficaciously formulated by ionotropic gelation technique with sustained release characteristics.

Keywords: NSAIDs, Alginate beads, cycloxygenase, Ionotropic gelation, Guar gum