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A Core Cross‐ L inked Polymeric Micellar Platium( IV ) Prodrug with Enhanced Anticancer Efficiency
Author(s) -
Hou Jie,
Shang Jincai,
Jiao Chengbin,
Jiang Peiyue,
Xiao Huijie,
Luo Lan,
Liu Tongjun
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.201300057
Subject(s) - prodrug , cisplatin , conjugate , chemistry , cytotoxicity , micelle , combinatorial chemistry , in vitro , cancer cell , biophysics , pharmacology , biochemistry , organic chemistry , cancer , chemotherapy , biology , mathematical analysis , mathematics , aqueous solution , genetics
A core cross‐linked polymeric micellar cisplatin(IV) conjugate prodrug is prepared by attaching the cisplatin(IV) to mPEG‐ b ‐PLL biodegradable copolymers to form micellar nanoparticles that can disintegrate to release the active anticancer agent cisplatin(II) in a mild reducing environment. Moreover, in vitro studies show that this cisplatin(IV) conjugate prodrug displays enhanced cytotoxicity against HepG2 cancer cells compared with cisplatin(II). Further studies demonstrate that the high cellular uptake and platinum‐DNA adduct of this cisplatin(IV) conjugate prodrug can induce more cancer‐cell apoptosis than cisplatin(II), which is responsible for its enhanced anticancer activity.