Formulation and In-Vitro Evaluation of Liposomal Drug Delivery System of Cabazitaxel

Abstract

Formulation and In-Vitro Evaluation of Liposomal Drug Delivery System of Cabazitaxel Cabazitaxel is a semi-synthetic derivative of a natural taxoid and is used for the treatment of advanced prostate cancer. In the present study Cabazitaxel liposomes were prepared by thin film hydration technique using lecithin, cholesterol, and Tween 80. Six formulations of liposomes were evaluated for physico chemical properties and in vitro drug release. The compatibility of drug with other ingredients was checked by FTIR studies. The prepared liposomes were characterized for surface morphology by SEM analysis, Percentage drug entrapment efficiency, Particle size, and Zeta potential analysis. The in-vitro drug release for optimized formulation F2 followed zero-order release kinetics. F2 was formulated using 270 mg lecithin and 30 mg cholesterol and 0.5 ml of Tween 80 with an objective to achieve a linear release profile for 24 hr. There was no initial burst release, with 5.68% of drug released during the first hour and release was extended up to 24 hrs. Study of drug release kinetics was performed by application of in-vitro drug release data to various kinetic equations like zero-order; first order, Higuchi and Korsmeyer-Peppas and from ‘n’ value (1.515) it was concluded that the drug release followed zero order kinetics with super case-II transport which indicates both erosion and diffusion as the release mechanisms. Stability studies at different temperatures were conducted and maximum drug retention was found at refrigerated temperature 4oC.