Development of a Novel Controlled Release System for Gastric Retention

Abstract

The present study reports the development of a novel multiple-unit floating dosage form for aceclofenac based on an emulsion solvent diffusion technique. There were two principle objectives to this study. Firstly, the suitability of different polymer such as Eudragit S 100, Eudragit RL 100, ethyl cellulose and HPMC either alone or in combination for the production of floating microspheres were investigated. The second objective was to assess the effect of stirring speed on various physiochemical properties of prepared floating microspheres. The size of the microspheres formed may however be a function of many factors such as stirring speed, viscosity of the dispersed phase, dispersion medium and temperature etc. Therefore, it is possible to prepare microspheres of desired size by varying some of these parameters. From the literature review, it was found that entrapment efficiency, particle size, floating ability, and drug release of floating microspheres could be adjusted by altering the stirring rate during microencapsulation. The floating microspheres of aceclofenac prepared by emulsion solvent diffusion method exhibited excellent in vitro buoyancy and zero order drug release. The surface response central composite design methodology could be successfully employed for assessing the influence of formulation parameters on the desired response. The drug polymer concentration and stirring rate played a vital role in achieving the desirable designed product. In all in vivo study, formulation was found to be superior. Hence, the floating hollow microspheres of aceclofenac prepared with acrylic polymers may provide a convenient dosage form for achieving better floating and drug release. It can be concluded that, A novel floating drug delivery system of aceclofenac can be formulated as an approach to increase gastric residence time and thereby improve its bioavailability. Among the polymers used the combination of Eudragit S 100 and Eudragit RL 100 showed better control over drug release and floating ability.