Chin. J. Org. Chem. ›› 2013, Vol. 33 ›› Issue (12): 2520-2527.DOI: 10.6023/cjoc201310043 Previous Articles     Next Articles



蔡晓冰a, 胡薇b, 陆国林c, 黄晓宇c   

  1. a 同济大学附属上海第十人民医院骨科 上海 200072;
    b 第二军医大学附属长海医院普四科 上海 200433;
    c 中国科学院上海有机化学研究所 上海 200032
  • 收稿日期:2013-10-26 修回日期:2013-11-11 发布日期:2013-11-14
  • 通讯作者: 胡薇, 黄晓宇;
  • 基金资助:

    国家自然科学基金(Nos. 81171737,21174158)资助项目.

Synthesis of PPEGMEA-g-PBLG Amphiphilic Graft Copolymer and Its Research as Doxorubicin Delivery Vectors

Cai Xiaobinga, Hu Weib, Lu Guolinc, Huang Xiaoyuc   

  1. a Department of Orthopedics, Shanghai Tenth People's Hospital, Tongji University School of Medicine, Shanghai 200072;
    b Department of General Surgery, Changhai Hospital, Second Military Medical University, Shanghai 200433;
    c Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032
  • Received:2013-10-26 Revised:2013-11-11 Published:2013-11-14
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 81171737, 21174158).

The poly[poly(ethylene glycol) methyl ether acrylate] (PPEGMEA) backbone was first prepared by single electron transfer-living radical polymerization (SET-LRP). The backbone was treated with lithium diisopropylamide (LDA) and 2-bromoisobutyryl bromide at -78 ℃ to give Br-containing PPEGMEA-Br. PPEGMEA-NH2 macroinitiator was then prepared by successive substitution and reduction reactions. A series of well-defined PPEGMEA-g-PBLG graft copolymers were synthesized by ring-opening graft polymerization of γ-benzyl-L-glutamate-N-carboxyanhydride (BLG-NCA) via grafting-from technique. A series of doxorubicin (DOX)-loaded polymeric micelles based on PPEGMEA-g-PBLG amphiphilic graft copolymers were prepared. The drug loading content (DLC) was measured by UV and the DLC of polymeric micelles was found to be as high as 32.3%. The drug release in vitro showed good delayed drug release feature.

Key words: amphiphilic graft copolymer, single electron transfer-living radical polymerization, doxorubicin, drug carrier