Abstract

We encapsulated vincristine into folic acid-conjugated PEGylated liposomes to improve the anti-tumor efficacy on multidrug resistant cancers. It was observed that the drug delivery system we constructed exhibited maximum cytotoxicity on KBv200 cells (multidrug resistant variant) compared with any other formulations. The semi-quantitative analysis of region of interest revealed that there was a great increase in area under curve (AUC) of a near-infrared fluorescein in solid tumors due to folic acid-mediated accumulation. Folic acid-conjugated PEGylated liposomes showed a significant tumor growth inhibiting effect in vitro and in vivo. TUNEL assay revealed that folic acid-conjugated PEGylated liposomes could induce cell apoptosis much more greatly than others. This study demonstrated that it had potential application prospective for the treatment of multidrug resistant cancer.

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