γ-环糊精金属有机骨架材料提高难溶性药物二氟尼柳的溶出速率.PDFVIP

药学学报 Acta Pharmaceutica Sinica 2019, 54(1): 29 −35 ·29 · γ-环糊精金属有机骨架材料提高难溶性药物二氟尼柳的溶出速率 * 吴碧湲, 周奕先, 潘 昕, 权桂兰, 吴传斌 ( 中山大学药学院, 广东广州510006) 摘要: 本研究的目的是合成生物相容性优良的新型多孔材料γ-环糊精金属有机骨架(γ-cyclodextrin metal-organic framework, CD-MOF), 并探究其作为药物载体改善难溶性药物体外释放行为。通过γ-环糊精与钾离子的分子自组 装效应堆积形成骨架结构, 并调控晶体的生长速率, 得到不同粒径的CD-MOF 。以难溶性药物二氟尼柳(diflunisal, DIF) 为模型药物, 利用浸渍法将药物装载至CD-MOF 的孔道。采用扫描电镜、粉末X-射线衍射、N2 吸附-解吸附、 傅里叶红外光谱和热重分析等方法对不同尺寸多孔材料进行表征, 并考察载体的细胞毒性和提高难溶性药物溶出 速率的能力。实验结果表明, 合成的CD-MOF 呈孔道多样的立方体形貌、粒径均一、比表面积大和细胞毒性小。药 物负载前后载体的形貌和晶型均未改变, 难溶性药物二氟尼柳的溶解度和溶出速率显著提高。 关键词: 环糊精; 金属有机骨架材料; 溶解度; 难溶性药物; 二氟尼柳 中图分类号: R943 文献标识码: A 文章编号: 0513-4870(2019)01-0029-07 Improving the dissolution rate of water-insoluble diflunisal by γ-cyclodextrin metal-organic framework * WU Bi-yuan, ZHOU Yi-xian, PAN Xin, QUAN Gui-lan , WU Chuan-bin (School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China) Abstract : The aim of this study is to prepare porous γ- cyclodextrin metal-organic framework (CD-MOF) with good biocompatibility to improve the in vitro release properties of water-insoluble drugs. Different sizes of CD-MOF were obtained by controlling the self-assembly of γ- cyclodextrin and potassium ion and the rate of crystal growth. The poorly water-soluble diflunisal (DIF) was selected as the model drug and loaded into the interior of porous CD-MOF by the impregnation method. The DIF loaded CD-MOF (DIF-MOF) was characterized by