Development of pioglitazone hydrochloride lipospheres by melt dispersion technique: Optimization and evaluation

Abstract

The objective of the present study was to develop and evaluate pioglitazone hydrochloride loaded lipospheres for treatment of diabetes. Pioglitazone hydrochloride lipospheres were formulated by using melt dispersion (homogenization) technique using compritol 888 ATO as lipid matrix and Phospholipon 90G (P 90G), PVA, Poloxamer 188 as surfactants. Formulation was optimized by using 3 2 full factorial design where entrapment efficiency and particle size were dependent variables and lipid and surfactant concentration were independent variables. Optimized formulation of pioglitazone hydrochloride (PLS 5) shows 79.69 1.35% entrapment efficiency, 94.63 2.10% drug content and particle size was found to be 23.74 0.35m with spherical shaped free flowing particles. In vitro release was carried out using dissolution apparatus in 0.1N HCl and optimized formulation shows 96.06 0.54 % drug release within 8 hrs. which follows quasi-fickian type of transport and was characterized by the Korsmeyer-Peppas model. Formulation was stable at 5 o C 3 o C for two months. Developed liposphere formulation was able to sustain the drug release and entrap the pioglitazone hydrochloride drug at high level.