DESIGN PREPARE AND EVALUATION OF EZETIMIBE SELF EMULSIFYING DRUG DELIVERY SYSTEM

The composition of Ezetimibe loaded loaded SEDDS was optimized using 3² facorial design. The impact of the formulation parameters on mean globule size and percentage drug load were studied by applying the analysis of variance and regression models. Several formulation and process variables were evaluated and optimized by response surface methodology. The optimum formulation was prepared by response optimizer through desirability function and the experimental values were found to be in close agreement with the predicted values. Optimized formulation was further subjected to stability studies. Optimal Ezetimibe SEDDS contains sunflower oil as oil phase, labrasol as a surfactant and transcutol HP as cosurfactant (Smix) in the ratio of 67.586% oil and 52.529% % w/w Smix formulates SEDDS with lower droplet size (169.7nm), PDI (0.2), and zeta potential (-31.8 mv) and percentage drug load (87.2%) values.. It was concluded that the smaller particle size and drug load more the release of drug which results in better bioavailability. The in vitro evaluation parameters such as emulsification time, viscosity determination, cloud point measurement, turbidity measurement, refractive index and spectroscopic optical clarity test were performed and the results were found within the limits for all formulations of two drugs. The stability studies revealed that there was no change in particle size and percentage drug load for the two drugs after 6 months. The in vitro drug release from optimized Atorvastatin SEDDS formulation were found to be 99.75% after 90 min. It was extremely higher in comparison to the marketed formulation and API suspension. In-vitro drug release studies closely indicate that optimized formulations obey first order kinetics and the mechanism of drug release was by fickian diffusion. The results further concluded that SEDDS can be explored as a potential drug carrier for dissolution enhancement of Atorvastatin other poorly soluble drugs.

Key words: Design Prepare, Evaluation, Ezetimibe, Self-Emulsifying Drug Delivery System