Preparation, optimization, and In vitro drug release study of microemulsions of posaconazole

Abstract

Self-emulsifying drug delivery systems (SEDDS) are novel carriers that could be used to improve the oral bioavailability of drugs with low water solubility. This study aims to develop stable microemulsions (MEs) as SEDDS that enhance the oral bioavailability of posaconazole (PSC) (BCS Class II compound). The other objective of this study was to optimize the impact of various factors affecting the formation, physicochemical characteristics, and stability of PSC-loaded SEDDS.The MEs were formed by mixing oil, surfactants, and cosurfactants based on the water titration approach. Different formulations were made and studied to characterize each formulation. In the optimization of the ME composition, the solubility study of PSC and the triangular phase diagram with various components (i.e., oils, surfactants, and co-surfactants) were taken into consideration. After selecting the best formulations, their physicochemical properties, including average particle size, polydispersity index, zeta potential, formulation stability, and turbidity, were investigated. Finally, the formulations were used for invitro drug release study. The results of this work prove that the selection of proper combinations of components allows for reaching drug-controlled delivery formulation. Additionally, the drug's effectiveness is enhanced with the optimization and development of SEDDS so that it reduces the total dose, thereby minimizing its side effects.