Formulation and Evaluation of Fluconazole Microsponge using Eudragit L 100 by Quasi Emulsion Solvent Diffusion Method

摘要

The aim of the present study is to formulate and evaluate the fluconazole microsponge by using Eudragit L 100. Microsponge was made because they provide controlled as well as target specific release of the drug. Thus study the effect of stirring rate on the formation of microsponge. Microsponge containing Fluconazole were prepared by quasi-emulsion solvent diffusion method at different stirring rate i.e 500, 800, 1000, 1200 and 1500 rpm. Particle size of prepared microsponge was observed in the range of 76.2 to 32.5μm. Scanning electron microscopy revealed the porous, spherical nature of the microsponges. The production yield, entrapment efficiency and drug content were found to be 78.24%, 82.76%, 81.36%. The impact of Drug: Polymer ratio and process variables i.e stirring speed and stirring time on the physical features of microsponges like production yield, mean particle size, entrapment efficiency were examined. It was shown that production yield, drug content and entrapment efficiency was found to be increase with increase in drug polymer ratio while drug: polymer ratio has reverse effect on particle size, as drug: polymer ratio increase, particle size decrease. As the polymer concentration increased, more amount of polymer surrounding the drug, thus increasing the thickness of the wall of the polymer matrix which lead to extended diffusion path and ultimately to lesser drug release or more sustained release. The effect of stirring rate on the morphology of microsponge. The formulation with higher drug to polymer ratio 1:8 (i.e F4) was chosen to investigate the effect of stirring rate on the morphology of microsponges. The dispersion of the drug and polymer within the aqueous phase was found to be dependent on the agitation speed. As the speed was increased the size of microsponges was reduced and the microsponges were found to be spherical and uniform.