金属有机骨架MIL-53装载抗肿瘤药氟尿嘧啶的基础研究  

Investigation of Anticancer Drug 5-Fu Loaded Porous Metal-Organic Frameworks of MIL-53

作　　者：杨宝春[1] 陈志良[2] 邹尚荣[1] 姜耀东[3] 任非[2] 

机构地区：[1]广州市第八人民医院药剂科,广州510060 [2]南方医科大学南方医院药学部,广州510515 [3]南方医科大学南方医院泌尿外科,广州510515

出　　处：《中国药学杂志》2014年第2期129-133,共5页Chinese Pharmaceutical Journal

基　　金：南方医院院长基金资助(2009C012)

摘　　要：目的研究金属有机骨架MIL-53作为药物载体装载抗肿瘤药氟尿嘧啶(5-Fu),及其体外释药和MIL-53的细胞相容性。方法以水热法制备金属有机骨架MIL-53,并通过透射电镜(TEM),X-射线粉末衍射(XRD),红外光谱(IR),热重分析(TG)对所得样品进行表征。以氟尿嘧啶为模型药物,研究MIL-53载药、体外释药和载体MIL-53的细胞相容性。结果 X-射线粉末衍射谱图与红外光谱图确定了样品MIL-53的结构,透射电镜结果表明MIL-53粒径为纳米级,热重分析的结果表明制备的MIL-53热稳定性良好,MIL-53对氟尿嘧啶的最高载入量为0.431 g·g-1载体,载药体系的体外释药具有明显的两相模式。体外细胞毒性实验表明,MIL-53低浓度具有良好的生物相容性。结论 MIL-53具有大的孔隙,高的载药量和低浓度具有较好的生物相容性,有望成为药物载体。OBJECTIVE To study the drug release and cytotoxicity in vitro of 5-fluorouracil （5-Fu）-loaded porous metal-organic frameworks of MIL-53. METHODS MIL-53 was hydrothermally synthesized, and the synthetic MIL-53 was characterized by TEM, XRD, IR and TG. 5-Fu was loaded into MIL-53, and the release pattern and cytotoxicity were investigated. RESULTS The structure of MIL-53 was confirmed. The diameter of MIL-53 was at nanometer level and MIL-53 displayed better thermo-stabilization. The high- est drug loading rate was 0.431 g ~ g-~ MIL-53 for 5-Fu. The drug release profile of 5-Fu-loaded MIL-53 displayed a clear biphasic re- lease pattern. Cytotoxicity test showed that MIL-53 had good biocompatility at lower concentrations. CONCLUSION MIL-53 is a promising platform for drug delive T due to its large pore sizes for drug encapsulation and good biocompatility at lower concentrations.

关 键 词：金属有机骨架 氟尿嘧啶 载药量 细胞毒性 

分 类 号：R994[医药卫生—毒理学]