Formulation And Evaluation of Diclophenac HPMC Gelatin Microspheres

Abstract

Diclofenac sodium is a well-known representative of non-steroidal anti-inflammatory drugs (NSAIDs), widely used to suppress pain and inflammation of rheumatic and non-rheumatic origin. NSAID treatment has been observed to have gastrointestinal side effects. Formulation of diclofenac sodium using biodegradable and biocompatible microsphere polymers is expected to reduce GI side effects. In this study, various microsphere formulations of diclofenac sodium were prepared by ionotropic gelation technique using sodium alginate as a carrier and HPMC as a release modifying agent. The diclofenac sodium microspheres prepared in this study were evaluated for flow properties, drug entrapment efficiency and also drug release from various designed formulations. Controlled release diclofenac sodium microspheres were successfully prepared using the ionotropic gelation technique. The prepared formulations were found to control the release of the active substance for 12 hours when tested in phosphate buffer (pH 7.4). The obtained results proved the suitability of the prepared diclofenac sodium microspheres as controlled-release dosage forms. Flow characterization showed Hausner ratio < 1.25 and Carr index 5-13% of the prepared systems, while drug alone ratios were > 1.25 and > 40%, respectively, indicating good and excellent flow of the systems and extremely poor fluidity of the drug. alone. The content of diclofenac sodium in the different formulations was not affected by the type of polymer, nor by the ratio of drug to polymer, which ranged between 79-90%. The surface morphology of the drug-loaded microspheres prepared with sodium alginate and HPMC was spherical in shape and large bridges were observed on the outer surface. During the six-month stability testing period, there was no significant degradation of diclofenac sodium or change in drug release rate in any of the prepared formulations. In vitro release studies showed that the rate of drug release was modified. This study presents a novel approach to obtain a modified release drug delivery system for diclofenac sodium.