Preparation, characterization and in vitro cytotoxicity evaluation of docetaxel nanoparticles against A549 cell line

Introduction: Docetaxel (DTX) is one of the most potent anticancer drugs in the taxane family. The commercial formulation of DTX for clinical use consists of high concentrations of tween80, which has been caused serious patient`s difficulties. Therefore, preparation of novel drug delivery system with ability of removing tween 80 and targeting on cancer tissue can lead more effective and also decrease side effects. This study is focused on preparation, characterization and cytotoxicity evaluation of docetaxel and poly lactic-co-glycolic acid (PLGA) nanoparticles (NPs) against a tumor cell line. Materials and Methods: NPs of DTX and PLGA was prepared by a modified emulsification/solvent diffusion method. Then the obtained NPs were characterized and evaluated. For this purpose, 10000 viable cells were seeded in each well of 96-well plate and after 24 hours of incubation different concentrations of conventional and NPs were added to the wells. Then mitochondrial dehydrogenase activities in living cells were determined at 24, 48 and 72 hours by MTT assay. Results: The average diameter of the NPs was approximately 184.3 ± 14.6 nm with poly dispersity index of 0.15. Notably, the results showed significant increase in cytotoxicity of the NPs against the A549 cell line. Inhibitory concentration (IC50) of free drug and NPs was 20.66 ± 0.22, 18.27 ± 0.45, 10.64 ± 0.38 and 0.57 ± 0.04, 0.16 ± 0.04, 0.07 ± 0.01 (µg/ml) at 24, 48 and 72 hours respectively. Conclusion: This study demonstrates the higher cytotoxicity of DTX-PLGA NPs on human lung cancer cell line. The present formulation can be considered for the further studies on other cell lines and in vivo evaluation.