Premium
Poly( L ‐aspartamide)‐ B ased Reduction‐ S ensitive Micelles as Nanocarriers to Improve Doxorubicin Content in Cell Nuclei and to Enhance Antitumor Activity
Author(s) -
Cui Can,
Xue YaNan,
Wu Ming,
Zhang Yang,
Yu Ping,
Liu Lei,
Zhuo RenXi,
Huang ShiWen
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.201300031
Subject(s) - micelle , endocytosis , nanocarriers , chemistry , biophysics , hela , doxorubicin , intracellular , in vitro , aqueous solution , biochemistry , cell , drug delivery , organic chemistry , biology , chemotherapy , genetics
A reduction‐sensitive graft polymer PHEA‐S‐S‐C 16 with poly{ α , β ‐[ N ‐(2‐hydroxyethyl)‐ L ‐aspartamide]} (PHEA) as a backbone and a disulfide‐containing alkyl as a side chain (HOOC‐S‐S‐C 16 ) is synthesized and evaluated for intracellular DOX delivery. PHEA‐S‐S‐C 16 can self‐assemble into micelles in aqueous media and load DOX at a total content of 7.3%. In vitro release studies reveal that the release rate of DOX from PHEA‐S‐S‐C 16 micelles is accelerated in the presence of DTT. The results of cell experiments indicate that DOX‐loaded mPEG‐S‐S‐C 16 micelles can achieve rapid DOX release in HeLa cells, as compared with their reduction‐insensitive counterparts. Endocytosis inhibition analysis indicates that PHEA‐S‐S‐C 16 micelles entered cells mainly via clathrin‐mediated endocytosis.