Self Emulsifying Drug Delivery Systems (SEDDS) of Ezetimibe for Enhancement of Oral Bioavailability: Formulation, Optimization and Characterisation

Abstract

Ezetimibe is BCS class II drug with low water solubility and good permeability having Log P value 4.14. It exhibit very low bioavailability with high intersubject variability and lack of dose proportionality. Various formulation strategies have been tried for BCS class II drugs such as solid dispersion, complexation, lipid-based systems for improving their solubility and dissolution profile. In this research we tried lipid-based formulation called SEDDS for ezetimibe drug to enhance their bioavailability by improving its solubility. On the basis of UV, DSC & FTIR purity of drug was checked, after which saturation solubility studies of ezetimibe was done in numerous Oils, Surfactants and Co-surfactants for selection of all three components. The ratio of Smix was selected using ternary phase diagram using water titration method. Formulation was prepared using Capryol 90 as oil phase, Tween 80 as Surfactant and Transcutol P as Co-surfactant. Characterization was done on the basis of result, optimization was performed using simplex centroid design of Mixture design. The finding was to see the effect of each component with their ratio on self-emulsification process and to evaluate. The aim of the study was to formulate SEDDS with small droplet size to increase the bioavailability of ezetimibe in the body given by oral route of administration.