葛根素-大豆苷元包合物纳米晶的制备及性能研究  

Preparation and Performance Study of Puerarin Daidzein Inclusion Complex Nanocrystals

作　　者：叶盛航 朱卫丰 臧振中 周昌 陈海燕 董欢欢 管咏梅 YE Shenghang;ZHU Weifeng;ZANG Zhenzhong;ZHOU Chang;CHEN Haiyan;DONG Huanhuan;GUAN Yongmei(MOE Key Laboratory of Modern Preparation of Traditional Chinese Medicine,Jiangxi University of Chinese Medicine,Nanchang 330004,China;Jiangxi Medical College,Shangrao 334000,China;School of Pharmacy,Jiangxi University of Chinese Medicine,Nanchang 330004,China)

机构地区：[1]江西中医药大学,现代中药制剂教育部重点实验室,南昌330004 [2]江西医学高等专科学校,江西上饶334000 [3]江西中医药大学药学院,南昌330004

出　　处：《中国药学杂志》2024年第22期2159-2168,共10页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金项目资助(82260765);江西省科技厅揭榜挂帅项目资助(20223BBG71002);江西省重点研发计划(20224BBG71023);江西省高层次高技能领军人才培养工程(12623001);江西中医药大学大学生创新创业训练计划项目资助(JZYC22S72);葛根、粉葛的食疗健康产品开发转化(2017YFC1702900-202403)。

摘　　要：目的基于葛根黄酮类成分间溶解性和渗透性具有“自洽”作用,以聚乙二醇(PEG)和壳聚糖(CS)为载体材料进行葛根素-大豆苷元多孔纳米晶的制备,并评价其理化性质和体外特性。方法以载药率和包封率作为考察指标进行处方优化,通过两步法以包合物形式包裹难溶性药物葛根素-大豆苷元形成β-环糊精(β-CD)-葛根素-大豆苷元-PEG-CS纳米晶。采用傅里叶变换红外、热重、X射线衍射、扫描电子显微镜、抗氧化和抑菌性能测试等确定葛根素-大豆苷元纳米晶的包合程度,以证实制备方法的可行性。并考察其在释放介质pH值1.2、6.8和7.4磷酸盐缓冲溶液条件下的释药行为,并对释药模型进行拟合。结果饱和水溶液法制备的包合物在体积分数为1.000%乙酸配比下制成的包合物最佳。其累积释放率约为90%,载药量和包合率分别为(26.13±0.74)%、(78.39±2.23)%,葛根素-大豆苷元纳米晶孔径多而密,抗氧化性能良好,对大肠杆菌、金黄色葡萄球菌、铜绿假单胞菌均能观察到明显抑菌圈,显示出良好的抗菌性能。结论葛根素-大豆苷元多孔纳米晶可显著提高难溶性药物大豆苷元的溶出度,为其在生物医药领域的应用奠定了一定基础。OBJECTIVE To prepare puerarin/daidzein porous nanocrystals using polyethyleneglycol(PEG)and chitosan(CS)as carrier aterialsand evaluate their physicochemical properties and in vitro characteristics.METHODS The drug loading rate and entrapment rate were used as indicators to optimize the prescription,and the insoluble drug puerarin-daidzein was encapsulated in the form of inclusion compound by two-step methodβ-CD-puerarin-daidzein-PEG-CS nanocrystals.The inclusion degree of puerarin-daidzein nanocrystals was determined by Fourier transform infrared spectroscopy,thermogravimetry,X-ray diffraction,scanning electron microscope,antioxidant and bacteriostatic tests to verify the feasibility of the preparation method.And investigate its drug release behavior in simulated gastrointestinal fluid and gastric environment,and fit the drug release model.RESULTS The inclusion compound prepared by saturated aqueous solution method was the best when the volume fraction of inclusion compound was 1.000%acetic acid.Its cumulative release rate is about 90%,drug loading and inclusion rate are(26.13±0.74)%and(78.39±2.23)%,respectively.Puerarin-daidzein nanocrystals have many and dense pore diameters,and have good antioxidant performance.Obvious inhibition zone against Escherichia coli,Staphylococcus aureus,and Pseudomonas aeruginosa can be observed,showing good antibacterial performance.CONCLUSION Puerarin-Daidzein porous nanocrystals can significantly improve the dissolution of insoluble drug daidzein,which lays a foundation for its application in the field of biomedicine.

关 键 词：纳米晶 制备 表征 葛根素 大豆苷元 溶解度 生物利用度 

分 类 号：R944[医药卫生—药剂学]