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.
作者
陈敏燕
韩璐
王蓉
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)
出处
《中南药学》
CAS
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)。
