化学学报 ›› 2009, Vol. 67 ›› Issue (12): 1363-1369. 上一篇    下一篇

研究论文

PPEGMEA-g-PDEAEMA全亲水接枝共聚物的合成及其 包埋甲氨喋呤体外控释的研究

黄晓炜a 顾丽娜b 陆国林b 黄 啸*,a 张亚琴b 黄晓宇*,b

  

  1. (a复旦大学附属肿瘤医院妇科 复旦大学上海医学院肿瘤学系 上海 200032)
    (b中国科学院上海有机化学研究所 上海 200032)

  • 投稿日期:2009-02-16 修回日期:2009-03-17 发布日期:2009-06-28
  • 通讯作者: 黄晓宇

Synthesis of PPEGMEA-g-PDEAEMA Double Hydrophilic Graft Copolymer and Studies on Controlled Drug Release in vitro of Loaded Methotrexate

Huang, Xiaowei a Gu, Lina b Lu, Guolin b Huang, Xiao *,a
Zhang, Yaqin b Huang, Xiaoyu *,b
  

  1. (a Department of Gynecology, Cancer Hospital, Fudan University; Department of Oncology, Shanghai Medical College,
    Fudan University, Shanghai 200032)
    (b Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032)
  • Received:2009-02-16 Revised:2009-03-17 Published:2009-06-28
  • Contact: Huang, Xiaoyu

以聚乙二醇丙烯酸酯(PEGMEA)为起始原料, 将原子转移自由基聚合(ATRP)技术和从主干接枝(grafting-from)策略相结合, 合成了结构规整的聚甲基醚聚乙二醇丙烯酸酯-g-聚(N,N’-二乙基胺乙基甲基丙烯酸酯) (PPEGMEA-g- PDEAEMA)接枝共聚物. 这种接枝共聚物通过静电作用形成胶束包埋甲氨喋呤(MTX), 得到具有98.7%高包封率的药物载体, 体外药物释放得到很好的控制.

关键词: 全亲水接枝共聚物, 胶束, 药物控释

A well-defined poly[poly(ethylene glycol) methyl ether acrylate]-g-poly[(N,N’-diethylamino)-
ethyl methacrylate] (PPEGMEA-g-PDEAEMA) graft copolymer was synthesized by the combination of atom radical transfer polymerization (ATRP) and the grafting-from strategy using poly(ethylene glycol) methyl ether acrylate (PEGMEA) as starting material. PPEGMEA-g-PDEAEMA-based micelles formed by electrostatic complexes were employed to load methotrexate (MTX) with a high drug loading efficiency of 98.7% and the drug release in vitro was well controlled.

Key words: double hydrophilic graft copolymer, micelle, drug release