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

Langmuir. 2019 Jan 15;35(2):504-512. doi: 10.1021/acs.langmuir.8b03693. Epub 2019 Jan 2.

Abstract

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(ε-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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Biomimetic Materials / chemical synthesis
  • Biomimetic Materials / chemistry
  • Biomimetic Materials / toxicity
  • Cell Line, Tumor
  • Cell Membrane / chemistry
  • Doxorubicin / pharmacology*
  • Drug Carriers / chemical synthesis
  • Drug Carriers / chemistry*
  • Drug Carriers / toxicity
  • Folic Acid / chemistry*
  • Folic Acid / toxicity
  • Humans
  • Micelles*
  • Polymers / chemical synthesis
  • Polymers / chemistry*
  • Polymers / toxicity

Substances

  • Antineoplastic Agents
  • Drug Carriers
  • Micelles
  • Polymers
  • Doxorubicin
  • Folic Acid