高等学校化学学报 ›› 2005, Vol. 26 ›› Issue (2): 353.

• 研究论文 • 上一篇    下一篇

聚酰胺-胺(PAMAM)树状大分子对甲氨蝶呤的包合及缓释研究

叶玲1, 江晓舟1, 杨华1, 苏健婷1, 恽榴红2   

  1. 1. 首都医科大学化学生物学与药学院,北京 100054;
    2. 军事医学科学院毒物药物研究所,北京 100850
  • 收稿日期:2004-01-14 出版日期:2005-02-10 发布日期:2005-02-10
  • 通讯作者: 叶 玲(1963年出生),女,副教授,主要从事树状大分子药物载体的研究.E-mail:yelingw@sina.com E-mail:yelingw@sina.com
  • 基金资助:

    北京市科技新星(批准号:954812000);北京市教委科技发展计划项目(批准号:00KJ-107)资助.

Complex and in vitro Release of Methotrexate-PAMAM Dendrimer

YE Ling1, JING Xiao-Zhou1, YANG Hua1, SU Jian-Ting1, YUN Liu-Hong2   

  1. 1. Capital University of Medical Sciences, Beijing 100054, China;
    2. Academy of Military Medical Sciences, Beijing 100850, China
  • Received:2004-01-14 Online:2005-02-10 Published:2005-02-10

摘要: 以甲氨蝶呤(MTX)为模型药物,研究了G5.0PAMAM树状大分子对其包合和释放,并用13CNMR对PAMAM-MTX包合物进行了表征.UV-Vis研究结果表明,1个G5.0PAMAM树状大分子能包合27个MTX分子,体外释放研究表明,在37℃,pH=7.4的10mmol/LTris-HCl缓冲溶液中G5.0PAMAM树状大分子对MTX具有明显的缓释作用.

关键词: PAMAM树状大分子, 甲氨蝶呤(MTX), 包合, 缓释

Abstract: We investigated the interaction between G5.0 PAMAM and methotrexate(MTX) drug molecules by 13C NMR, and it has been proven that the interaction is occurring between the PAMAM amine functional groups and the MTX carboxyl groups. UV-Vis study showed each G5.0 PAMAM could conjugate up to 27 MTX molecules. The release of MTX from complex is much slower than that of free MTX at pH=7.4, 10 mmol/L Tris-HCl buffer. The presence of 0.02 mol/L NaCl in buffer increases the release rate of MTX from the complex, which further defines the interaction between PAMAM and MTX.

Key words: Polyamidoamine(PAMAM) dendrimer, Methotrexate(MTX), Release

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