期刊
JOURNAL OF CONTROLLED RELEASE
卷 105, 期 1-2, 页码 142-150出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.jconrel.2005.03.016
关键词
polyphosphazene; platinum conjugate; anticancer drug; tumor selectivity
A new amphiphilic poly(organophosphazene) was synthesized by stepwise nucleophilic substitutions with a hydrophilic methoxy poly(ethylene glycol) with an average molecular weight of 350 (MPEG350) and a hydrophobic glyCyl-L-glutamate as side groups, and then an antitumor (dach)platinum(II) (dach: trans -(+/-)- 1,2-diaminocyclohexane) moiety was conjugated to the polymer using the dipeptide as a spacer. This polymeric platinum conjugate was found to be accumulated in the tumor tissue to a remarkably greater extent than in the normal tissue (tumor/tissue ratio > 4), probably due to the excellent EPR effect and the long circulating properties of the polymer conjugate (t(1/2 beta)=6.2 h and AUC=4020 nmol h/ml) compared with carboplatin ((1/2 beta) =0.42 h and AUC=120 nmol h/ml). The polymer conjugate also exhibited high in vitro cytotoxicity comparable to cisplatin against several human tumor cells tested. (c) 2005 Elsevier B.V. All rights reserved.
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