NEW POLYMER-PLATINUM (Ⅱ) ANTITUMOR CONJUGATES
Cisplatin is widely used in clinical practice for many kinds of malignant tumors. But its side effects are serious, such as nephrotoxicity, cytotoxicity, and peripheral neuropathy. Great efforts have been made to reduce its toxic side effects and increase its efficacy, including developing other Pt(II) or Pt(IV) complexes and conjugating platinum complexes to water soluble PHPMA or poly(amino acid)s. In the present contribution, an amphiphilic biodegradable polymer with pendant carboxyl groups, MPEG-b-P(LA-co-MCC), was synthesized. Platinum complex (l,2-diaminocyclohexane)platinum(II) chloride (DACH-Pt) was reacted with the pendant COOH groups on MPEG-b-P(LA-co-MCC) to form a polymer-platinum conjugate. This conjugate can self-assemble into water soluble micelles. These micelles displayed dose-dependent cytotoxicity against human breast cancer EMT6 cells and their cytotoxicity was comparable to oxaliplatin. The Pt(II) complex was released from the micelles at pH 7.4 in a sustained manner.
biodegradable polymers platinum drug micelles
Haihua Xiao Yanyan Fan Shi Liu Xuesi Chen Yubin Huang Xiabin Jing
State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry,Chin State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry,Chin
国际会议
The First Symposium on Innovative Polymers for Controlled Delivery(新型高分子材料与控制释放国际会议 SIPCD 2010)
苏州
英文
267-269
2010-09-14（万方平台首次上网日期，不代表论文的发表时间）