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Self‐ A ssemblies of p H ‐ A ctivatable PEG ylated Multiarm Poly(lactic acid‐ co ‐glycolic acid)‐ D oxorubicin Prodrugs with Improved Long‐ T erm Antitumor Efficacies
Author(s) -
Ding Jianxun,
Li Di,
Zhuang Xiuli,
Chen Xuesi
Publication year - 2013
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.201300160
Subject(s) - prodrug , micelle , chemistry , ethylene glycol , peg ratio , plga , lactic acid , glycolic acid , in vitro , combinatorial chemistry , biophysics , biochemistry , organic chemistry , aqueous solution , finance , biology , bacteria , economics , genetics
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.