γ-环糊精-金属有机骨架负载黄芪甲苷的制备及其性质研究  

Preparation and properties of astragaloside loaded byγ-cyclodextrin metal-organic framework

作　　者：陈敏燕[1] 韩璐[1] 王蓉[1] 杨刚 CHEN Min-yan;HAN Lu;WANG Rong;YANG Gang(Department of Pharmacy,the Ninth People’s Hospital Affiliated to Medical School,Shanghai Jiao Tong University,Shanghai 200011)

机构地区：[1]上海交通大学医学院附属第九人民医院药剂科,上海200011

出　　处：《中南药学》2024年第5期1220-1226,共7页Central South Pharmacy

基　　金：国家自然科学基金青年科学基金项目(No.82204768)。

摘　　要：目的 以γ-环糊精-金属有机骨架(CD-MOF)为载体制备载黄芪甲苷(AST)的AST@CD-MOF并研究其对AST溶解度、溶出速率、稳定性及A549细胞凋亡的影响。方法 以溶剂孵育法将AST负载于CD-MOF中,采用环境扫描电子显微镜、氮气吸附脱附等手段表征AST@CD-MOF的形貌和吸附特性,同时对AST@CD-MOF的溶解度、溶出速率、稳定性及诱导A549细胞凋亡能力进行考察,并与环糊精包合物(AST@γ-CD)和原料药进行对比。结果 制备得到的AST@CD-MOF形貌呈均一的立方晶体,粒径约为140 nm,优化后的AST@CD-MOF载药量为(32.29±2.57)%,且具有良好的稳定性;AST@CD-MOF中AST的溶出速率和累计溶出百分率均得到显著提升,在6 h内的累计释放率达到80%以上;AST@CD-MOF诱导细胞的总凋亡比率可达68.18%,显著高于游离AST和AST@γ-CD。结论 CD-MOF显著提高了AST的水溶性和溶出速率,增强了AST诱导A549细胞凋亡的能力。Objective To prepareγ-cyclodextrin metal-organic framework(CD-MOF)containing astragaloside(AST)with CD-MOF as the carrier and to determine its effect on AST solubility,dissolution rate,stability and apoptosis of A549 cells.Methods AST was loaded into CD-MOF by solvent incubation method.The morphology and adsorption properties of AST@CD-MOF were characterized by environmental scanning electron microscopy and nitrogen adsorption.Meanwhile,the solubility,dissolution rate,stability and induction of A549 cell apoptosis of AST@CD-MOF were measured before comparion with those of AST@γ-CD and AST powder.Results The morphology of AST@CD-MOF was homogeneous cubic crystal with a particle size of about 140 nm.The drug loading of optimized AST@CD-MOF was(32.29±2.57)%,with good stability.The dissolution rate and cumulative dissolution rate of AST in AST@CD-MOF was obviously improved,and the cumulative dissolution percentage reached over 80%within 6 h.The total apoptosis rate induced by AST@CD-MOF was 68.18%,much higher than that induced by free AST and AST@γ-CD.Conclusion CD-MOF can greatly increase the water solubility and dissolution rate of AST,and enhance the ability of AST to induce the apoptosis of A549 cells.

关 键 词：黄芪甲苷 γ-环糊精-金属有机骨架 体外溶出 细胞凋亡 

分 类 号：R94[医药卫生—药剂学]