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Macromol Biosci. 2014 Sep;14(9):1280-90. doi: 10.1002/mabi.201400162. Epub 2014 May 28.

Charge-conversional and pH-sensitive PEGylated polymeric micelles as efficient nanocarriers for drug delivery.

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  • 1Department of Biomass Chemistry and Engineering, National Engineering Laboratory for Clean Technology of Leather Manufacture, Sichuan University, Chengdu, 610065, China.


A novel amphiphilic copolymer, poly (ethylene glycol)-graft-polyethyleneimine/amide (PEG-g-PEI/amide), is synthesized by grafting PEG and1,2-cis-Cyclohexanedicarboxylic anhydride onto the PEI. PEGylated polymeric micelles can be assembled from the amphiphilic copolymers with well-defined nano-sizes, and anti-cancer drugs are successfully loaded into micelle core formed by the amide. The amides with neighboring carboxylic acid groups exhibit pH-dependent hydrolysis and can reversibly shield the cationic charge of amine groups on the PEI, giving the micelles a charge-conversion property from negative to positive in acidic tumor tissue environment. Meanwhile, the cleavage of amide bonds at acidic pH also results in the disassembly of the micelle and pH-responsive drug release. These micelles are promising drug delivery systems due to their smart properties: PEGylation, suitable size, charge-conversion, and simultaneous pH-sensitive drug release.

© 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.


PEGylation; charge conversion; drug delivery; pH-sensitive; polymeric micelle

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