A pH-Sensitive Phospholipid Polymeric Prodrug Based on Branched Polyethylenimine for Intracellular Drug Delivery

A biomimic pH-sensitive polymeric prodrug based on branched polyethylenimine- graft -12-acryloyloxy dodecyl phosphorylcholine and 6-maleimidocaproyl-doxorubicin is rationally designed and successfully synthesized. This polymeric prodrug can spontaneously self-assemble into spherical nanostructures in aqueous solution. The in vitro drug release results imply that this polymeric prodrug can maintain stable in blood circulation while enhance drug release at endosomal acidic condition. Fluorescence microscopy and flow cytometry results demonstrate that the formed prodrug micelles can be internalized by cancer cells effectively. More importantly, this prodrug exhibits excellent cytotoxicity against Hela cells, indicating the pH-sensitive polymeric prodrug micelles can potentially work as a promising platform for efficient cancer therapy.