Self-assembled mPEG-PCL-g-PEI micelles for simultaneous codelivery of chemotherapeutic drugs and DNA: synthesis and characterization in vitro

Int J Nanomedicine. 2012:7:1749-59. doi: 10.2147/IJN.S28932. Epub 2012 Mar 30.

Abstract

Background: In this paper, a series of amphiphilic triblock copolymers based on polyethylene glycol-poly ɛ-caprolactone-polyethylenimine (mPEG-PCL-g-PEI) were successfully synthesized, and their application for codelivery of chemotherapeutic drugs and DNA simultaneously was investigated.

Methods and results: These copolymers could self-assemble into micelles with positive charges. The size and zeta potential of the micelles was measured, and the results indicate that temperature had a large effect on the micelles obtained. In vitro gene transfection evaluation in cancer cells indicated that the self-assembled micelles could serve as potential gene delivery vectors. In addition, hydrophobic drug entrapment efficiency and codelivery with the gene was also studied in vitro. The self-assembled micelles could load doxorubicin efficiently and increase cellular uptake in vitro, while maintaining high gene transfection efficiency.

Conclusion: The triblock copolymer mPEG-PCL-g-PEI could be a novel vector for codelivery of drug and gene therapy.

Keywords: DNA; drug codelivery; gene transfection; self-assembly; triblock copolymer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage*
  • Cell Line
  • DNA / administration & dosage*
  • DNA / genetics
  • Doxorubicin / administration & dosage
  • Drug Carriers / chemistry
  • Drug Delivery Systems
  • Genetic Therapy
  • HEK293 Cells
  • Humans
  • Mice
  • Micelles
  • Microscopy, Atomic Force
  • Microscopy, Electron, Transmission
  • Nanocapsules / chemistry
  • Nanocapsules / ultrastructure
  • Nanomedicine
  • Polyesters / chemistry
  • Polyethylene Glycols / chemistry
  • Polyethyleneimine / chemistry
  • Transfection

Substances

  • Antineoplastic Agents
  • Drug Carriers
  • Micelles
  • Nanocapsules
  • Polyesters
  • methoxy poly(ethylene glycol-co-epsilon-caprolactone)
  • Polyethylene Glycols
  • Doxorubicin
  • Polyethyleneimine
  • DNA