期刊
REACTIVE & FUNCTIONAL POLYMERS
卷 73, 期 3, 页码 564-572出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.reactfunctpolym.2012.12.012
关键词
Doxorubicin; Drug delivery; Folate; pH-sensitive; Polymeric micelles
资金
- National Natural Science Foundation of China [20974052]
- National Key Technologies R & D Program for New Drugs of China [2009ZX09301-002]
- Natural Science Foundation of Tianjin Municipality [09JCZDJC22900]
Folate-conjugated micelles were fabricated from amphiphilic diblock copolymers with poly(ethylene glycol) as the hydrophilic block and a random copolymer of n-butyl methacrylate and methacrylic acid as the hydrophobic block. Doxorubicin (DOX), a model drug that contains an amine group and hydrophobic moiety, was loaded with a high loading capacity into micelles by a combination of ionic bonding and hydrophobic effect. The combined interactions imparted a pH-sensitive delivery property to the system. The release rate of loaded DOX was slow at pH 7.4 (i.e., mimicking the plasma environment) but increased significantly at acidic pH (i.e., mimicking endosome/lysosome conditions). Acid-triggered drug release resulted from the carboxylate protonation of poly(methacrylic acid), which dissociated the ionic bonding between the micelles and DOX. Cellular uptake by folate receptor-overexpressing HeLa cells of the DOX-loaded folate-conjugated micelles was higher than that of micelles without folate conjugation. Thus, the DOX-loaded folate-conjugated micelles displayed higher cytotoxicity to HeLa cells. (C) 2013 Elsevier Ltd. All rights reserved.
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