Antitumor activity of transferrin-modified- artemether lipid nanospheres in cancer cell lines

Diverse lines of research show that the cellular response to artemether (ART) is multi-factorial in nature. The cytotoxicity of ART is specific to cancer cells because most of them over expressed; transferrin receptors and have high level of intracellular iron and ART is mainly toxic after; interaction with iron ion. Our aim is to investigate the effect of some formulation characteristics on; the cytotoxicity of ART in C6 and MCF-7 cells lines. In this study, the cytotoxicity of ART-loaded; anionic, cationic or neutral (transferrin modified) lipid nanospheres was studied by MTT and; apoptosis tests. Characterizations of apoptosis were done. The effect on the mitochondria and the; nucleus was qualitatively characterized after using different types of cell tracker dyes. The cellular; uptake, accumulation and distribution of the formulations were characterized after loading; different hydrophobic fluorescence probes instead of ART. The relation between the; accumulated amount of ART and its cytotoxicity was defined. Our study shows that ART can be highly toxic to the tumor cells if accumulated in a large amount in the cell. Lipid nanosphere containing tween80 and transferrin can highly accumulate ART in brain cells and can be; formulated as a promising potent, safe and inexpensive drug carriers for brain tumors. Schematic representation of cellular uptake and accumulation of artemether loaded in different types of lipid nanospheres, cationic, SA-LNS; Anionic, ART-LNS and Neutral-Targeted, TR-LNS. [Display omitted]