FORMULATION DEVELOPMENT AND EVALUATION OF TEMOZOLOMIDE LOADED HYDROGENATED SOYA PHOSPHATIDYLCHOLINE LIPOSOMES FOR THE TREATMENT OF BRAIN CANCER

Objective: The objective of this study was to encapsulate temozolomide (TMZ) in the liposomal formulation for the treatment of glioblastoma. TMZ is one of the most effective substances in vitro against cells derived from glioblastoma. However, it may not have a significant effect in vivo due to poor penetration in brain which may be attributed to the blood-brain-barrier. The main objective of this investigation is to develop a liposomal drug delivery system which could improve the brain targeting, and solve the treatment-related problems. Methods: In this study, TMZ loaded liposomes were prepared by ethanol injection method. The characterization of formulated liposomes was carried out by vesicle size, entrapment efficiency, surface morphology, and in vitro drug release study. The prepared liposomes were also evaluated for cell uptake and cell cytotoxicity studies. Results: Particle size and entrapment efficiency were found to be 105.7±3.9 nm and 78.25±0.98%, respectively. 75% of the entrapped drug was released in 24 hrs from the selected liposomal formulation. Cell uptake study reveals that hydrogenated soya phosphatidylcholine (HSPC) loaded TMZ liposomes interact with the glioblastoma cells and kill the cancer cells effectively. Cytotoxicity assay confirms that drug loaded HSPC liposomes are more efficient with respect to killing of glioblastoma cells as compared to plain drug. Conclusion: These results suggest that the TMZ loaded HSPC liposome may serve as a proficient targeted drug delivery system for the effective management of glioblastoma. Keywords: Temozolomide, Liposomes, Hydrogenated soya phosphatidylcholine, Cholesterol, Glioblastoma.