A pH‐Sensitive Phospholipid Polymeric Prodrug Based on Branched Polyethylenimine for Intracellular Drug Delivery. Issue 18 (16th August 2016)

• Record Type: Journal Article
• Authors: Wang, Haibo; Xiong, Junjie; Liu, Gongyan; Wang, Yunbing
• Is Part Of: Macromolecular chemistry and physics. Volume 217:Issue 18(2016:Sep.)
• Page Start: 2049
• Page End: 2055
• Publication Date: 2016-08-16
• Subjects: biomimic -- intracellular drug delivery -- pH‐responsive -- self‐assemble; Polymers -- Periodicals; Polymerization -- Periodicals; Synthetic products -- Periodicals; Macromolecules -- Periodicals; 547.7
• DOI: 10.1002/macp.201600261
• Languages: English
• ISSNs: 1022-1352

Abstract

Abstract : 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. Abstract : A biomimic pH‐sensitive polymeric prodrug based on branched polyethylenimine‐ graft ‐12‐acryloyloxy dodecyl phosphorylcholine and 6‐maleimidocaproyl‐doxorubicin is developed successfully. This polymeric prodrug can assemble into micelles with phosphorylcholine shells in aqueous solution and is stable in the physiological environment. Moreover, doxorubicin can be released from the prodrug micelles upon cancer cell intracellular acidic stimulus, which inhibits the proliferation of cancer cells efficiently.