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Charge‐Conversional and pH‐Sensitive PEGylated Polymeric Micelles as Efficient Nanocarriers for Drug Delivery
Author(s) -
Liu GongYan,
Li Min,
Zhu CongShan,
Jin Qiao,
Zhang ZongCai,
Ji Jian
Publication year - 2014
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.201400162
Subject(s) - micelle , nanocarriers , chemistry , amphiphile , pegylation , ethylene glycol , cationic polymerization , copolymer , polymer chemistry , amide , drug delivery , peg ratio , organic chemistry , polymer , aqueous solution , polyethylene glycol , finance , economics
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.