Folate-Conjugated Cell Membrane Mimetic Polymer Micelles for Tumor-Cell-Targeted Delivery of Doxorubicin

Tumor-targeting nano-drug-delivery systems hold great potential to improve the therapeutic efficacy and alleviate the side effects of cancer treatments. Herein, folic acid (FA)-decorated amphiphilic copolymer of FA-P(MPC-co-MaPCL) (MPC: 2-methacryloxoethyl phosphorylcholine, MaPCL: poly(epsilon-caprolactone) macromonomer) is synthesized and its micelles are fabricated for doxorubicin (DOX) delivery. And non-FA-decorated P(MPC-co-MaPCL) micelles are used as the control. Dynamic light scattering and scanning electron microscopy measurements reveal that FA-P(MPC-co-MaPCL) and P(MPC-co-MaPCL) micelles are spherical with average diameters of 140 and 90 nm, respectively. The evaluation in vitro demonstrates that the blank micelles are nontoxic, while DOX-loaded FA-P(MPC-co-MaPCL) micelles show significant cytotoxicity to HeLa cells and slight cytotoxicity to L929 cells. Moreover, the cellular uptake of DOX-loaded FA-P(MPC-co-MaPCL) micelles in HeLa cells are 4.3 fold and 1.7-fold higher than that of DOX-loaded P(MPC-co-MaPCL) micelles and free DOX after 6 h of incubation, respectively. These results indicate the great potential of this system in anticancer target drug-delivery applications.