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

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.