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Self-Assemblies of pH-Activatable PEGylated Multiarm Poly(lactic acid-co-glycolic acid)-Doxorubicin Prodrugs with Improved Long-Term Antitumor Efficacies†
Article first published online: 15 JUL 2013
© 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Volume 13, Issue 10, pages 1300–1307, October 2013
How to Cite
Ding, J., Li, D., Zhuang, X. and Chen, X. (2013), Self-Assemblies of pH-Activatable PEGylated Multiarm Poly(lactic acid-co-glycolic acid)-Doxorubicin Prodrugs with Improved Long-Term Antitumor Efficacies. Macromol. Biosci., 13: 1300–1307. doi: 10.1002/mabi.201300160
- Issue published online: 20 OCT 2013
- Article first published online: 15 JUL 2013
- Manuscript Revised: 4 MAY 2013
- Manuscript Received: 25 MAR 2013
- National Natural Science Foundation of China (Projects 51173184, 51021003, 51273196, 51203153, 21104076, 21004061, 51003103, 51273037, 21174142 and 51103015)
- malignancy therapy;
Two pH-activatable star-shaped prodrugs are synthesized through the condensation reaction between Y- or dumbbell-shaped poly(ethylene glycol)-poly(lactic acid-co-glycolic acid) (PEG-PLGA) copolymer and acid-sensitive cis-aconityl-doxorubicin. The prodrugs self-assemble into micelles with favorable hydrodynamic radii and relatively low critical micelle concentrations. In vitro DOX release from prodrug micelles is accelerated by the decrease of the PLGA content or at the late endosomal pH. The efficient cellular uptake and intracellular DOX release of the prodrug micelles are confirmed and the improved long-term anti-proliferative activities of prodrug micelles are revealed. These features suggest that the prodrugs provide a favorable approach to construct effective polymeric drug delivery systems for malignancy therapy.