高等学校化学学报 ›› 2012, Vol. 33 ›› Issue (01): 26-31.doi: 10.3969/j.issn.0251-0790.2012.01.004

• 研究论文: 无机化学 • 上一篇    下一篇

抗肿瘤药物在金属有机骨架中的装载及体外释放

杨宝春1, 姜耀东2, 秦雪娟1, 陈志良1, 任非1   

  1. 1. 南方医科大学南方医院药学部,
    2. 南方医院泌尿外科, 广州 510515
  • 收稿日期:2011-05-04 出版日期:2012-01-10 发布日期:2011-12-20
  • 通讯作者: 任非,女,博士,副主任药师,主要从事肿瘤药物纳米制剂相关的研究.E-mail:renfeisky@126.com E-mail:renfeisky@126.com
  • 基金资助:

    广东省科技计划(批准号: 2008B060600068)和南方医院院长基金(批准号: 2009C012)资助.

Loaded and in vitro Drug Release of Anticancer Drugs in Porous Metal-Organic Frameworks

YANG Bao-Chun1, JIANG Yao-Dong2, QIN Xue-Juan1, CHEN Zhi-Liang1, REN Fei1   

  1. 1. Department of Pharmacy,
    2. Department of Urology, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China
  • Received:2011-05-04 Online:2012-01-10 Published:2011-12-20
  • Contact: REN Fei E-mail:renfeisky@126.com

摘要: 以三乙胺直接加入法制备金属-有机骨架MOF-5, 采用X射线粉末衍射(XRD), 红外光谱(IR)和热重分析(TG)对所得样品进行表征. 分别以辣椒素和5-氟尿嘧啶(5-Fluouourail, 5-FU)为模型药物, 研究了MOF-5对2种药物的载药及体外释药性能. 通过将所得样品的XRD和IR谱图与标准谱图比对确定了样品的结构. TG结果表明, 所制备的MOF-5热稳定性良好. MOF-5对辣椒素的最高载入量达0.592 g/g载体, 对5-FU的最高载入量为0.315 g/g载体, 两种载药体系的体外释药均为明显的两相模式. 体外细胞毒性实验结果表明, MOF-5具有良好的生物相容性.

关键词: 金属-有机骨架, 辣椒素, 5-氟尿嘧啶, 载药量, 药物缓释, 细胞毒性

Abstract: Porous metal-organic frameworks(MOF-5) were synthesized and the structure of synthetic MOF-5 was confirmed by XRD and IR spectrum. According to the result of TG, the synthetic MOF-5 displayed better thermo-stabilization. The capsaicin or 5-fluouourail was loaded in synthetic MOF-5 and in vitro drug release profile were investigated, respectively. The highest drug loading rates are 0.592 g/g MOF for capsaicin and 0.315 g/g MOF for 5-FU in drug-loaded MOF-5, respectively. The in vitro drug release profile of both MOF-5 formulations showed a clear biphasic release pattern. Cytotoxicity test showed that MOF-5 displayed good biocompatility.

Key words: Metal-organic framework(MOF), Capsaicin, 5-Fluouourail(5-FU), Drug loading rate, Drug sustained release, Cytotoxicity

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