Development of Liposome Drug Delivery Systems for Anti-Glioma Therapy

Abstract

This study aims to investigate the potential of ethanol-based proliposomes in generating paclitaxel-loaded liposome delivery in vitro, by employing various phospholipid compositions.

Liposomes prepared using ethanol-based proliposome method successfully generated multilamellar vesicles. Three different lipid phases: SPC:Chol, HSPC:Chol or DPPC:Chol in 1:1 mole ratio were used in each liposomal formulation to compare their size, size distribution, zeta potential, pH and morphology. The size of the liposomes was then reduced into nanometre size range.

DPPC-liposomes entrapped 70-85% of the available paclitaxel compared to only 46-75% and 26-67% entrapped by liposomes made from SPC and HSPC respectively, using a range of paclitaxel concentration. The entrapment efficiency of liposomes was dependent on the lipid bilayer properties and ability of paclitaxel to modify surface charge.

In vitro studies revealed that paclitaxel alone was more toxic to U87-MG as well as SVG-P12 cell lines than liposome formulations. The cytotoxicity of liposomes was dependent on their entrapment efficiency and sustained drug release. Thus, DPPC-liposomes had a more cytotoxic effect on the cells than SPC and HSPC liposomes. However, Drug-free liposomes proved to be non-toxic to the cells, indicating that liposomes might enhance the efficacy of the entrapped drug. The properties of different liposome formulations were essential in understanding their drug delivery mechanism.