Abstract
Background and Objective: Reports revealed atorvastatin (ATR) exerts significant anti proliferative properties against cancer cell lines. Aim of this study was the potentiation of ATR cytotoxic effects against HepG2 cells by using TPGS as a surfactant and loading on PLGA NPs. Materials and Methods: Nanoprecipitation method was used to trap ATR within PLGA nanoparticles, the method uses vitamin E TPGS as an emulsifier. The nanoparticles' encapsulation efficiency, size, zeta potential (ZP), surface morphology and in vitro drug release were evaluated. Results: The mean size of the particles was 176.2 +/- 14.1 nm, they had a ZP of -15.1 +/- 4.4 mV and polydispersity index of 0.32 and after 12 h, approximately 96% of raw AIR had dissolved in comparing with 25% of raw ATR. It was found that ATR-NPs was twice as cytotoxic as the raw ATR. In both instances, for HepG2 cells cycle analysis accumulated at the pre-G1 apoptotic phase in response to ATR and ATR-NPs. Indeed, increase of cells at pre-G1 initiated by ATR 4.45 times the normal level, rising to a 24.05-fold increase for ATR-NPs. The ATR annexin V-FITC apoptosis assay showed significant increase in the amount of annexin V-FITC positive apoptotic cells (both early and late apoptosis) in HepG2 cells treated with ATR-NPs. Conclusion:These findings suggested that this formula is a promising therapy for patients with liver cancer.