Zwitterionic doxorubicin loaded micelles based on polyethyleneimine for enhanced antitumor therapy in vivo

Abstract

The development of biocompatible and efficient polymeric micelles for drug delivery has been drawing great attention. Herein, amphiphilic molecules (PMPC) were synthesized with zwitterionic linear polyethyleneimine (PEI) as the hydrophilic segment and mercapto-paclitaxel as the hydrophobic segment. The chemotherapeutic doxorubicin (DOX) was encapsulated in the PMPC micelles formed through self-assembly to prepare DOX-loaded micelles (PMPC–DOX micelles). The results showed that the prepared PMPC–DOX micelles exhibited good stability in protein solution. The release rate of DOX reached 48.12% within 36 h at pH 5.5. More importantly, the tumor targeting ability and the antitumor effect of PMPC–DOX micelles were better than those of free DOX, and the tumor inhibition rate of mice was 89.7% after 14 days of treatment. The as-prepared PEI-based drug-loaded micelles provide a new approach for the design of nanodrug delivery systems.