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. TMZis one of the most effective substances in vitro against cells derived from glioblastoma. However, it may not have a significant effect in vivo due topoor penetration in brain which may be attributed to the blood-brain-barrier. The main objective of this investigation is to develop a liposomal drugdelivery 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 carriedout by vesicle size, entrapment efficiency, surface morphology, and in vitro drug release study. The prepared liposomes were also evaluated for celluptake 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 wasreleased in 24 hrs from the selected liposomal formulation. Cell uptake study reveals that hydrogenated soya phosphatidylcholine (HSPC) loaded TMZliposomes interact with the glioblastoma cells and kill the cancer cells effectively. Cytotoxicity assay confirms that drug loaded HSPC liposomes aremore 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 effectivemanagement of glioblastoma.Keywords: Temozolomide, Liposomes, Hydrogenated soya phosphatidylcholine, Cholesterol, Glioblastoma