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

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

Macromolecular Bioscience 14(9): 1280-1290

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.

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Accession: 052042610

Download citation: RISBibTeXText

PMID: 24866398

DOI: 10.1002/mabi.201400162

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