苦参碱固体脂质纳米粒的构建及包封率测定方法研究  

Construction of Matrine Solid Lipid Nanoparticle and Determination of the Entrapment Efficiency

作　　者：靳雯臻 檀华进 汪凯康 谭晓川 张宇佳[1] 郑稳生[1] JIN Wen-zhen;TAN Hua-jin;WANG Kai-kang;TAN Xiao-chuan;ZHANG Yu-jia;ZHENG Wen-sheng(Institute of Materia Medica,Chinese Academy of Medical Sciences&Peking Union Medical College,Beijing City Key Laboratory of Drug Delivery Technology and Novel Formulation,Beijing 100050,China)

机构地区：[1]北京协和医学院中国医学科学院药物研究所,药物传输技术及新型制剂北京市重点实验室,北京100050

出　　处：《中国药学杂志》2020年第12期1015-1020,共6页Chinese Pharmaceutical Journal

基　　金：十三五重大新药创制科技重大专项项目资助(2018ZX09711001-002-005,2018ZX09721003-007-007);中国医学科学院医学与健康科技创新工程项目资助(2017-I2M-3-012)。

摘　　要：目的制备苦参碱固体脂质纳米粒并进行质量评价;利用不同方法测定苦参碱固体脂质纳米粒的包封率,建立其包封率测定方法。方法以微乳-探头超声法制备固体脂质纳米粒并对其粒径、电位、微观形态、体外释放等进行质量评价;建立苦参碱HPLC含量测定方法;分别采用葡聚糖凝胶法、低温超速离心法、超滤法、透析法测定苦参碱固体脂质纳米粒的包封率,比较各个方法的优点和缺点,筛选并建立有效测定包封率的方法。结果苦参碱固体脂质纳米粒粒径为(116.7±2.6)nm,Zeta电位为(-45±1.7)mV,透射电镜照片显示固体脂质纳米粒大小均一,形状为球形;体外释放结果显示,纳米粒呈现一定程度的缓释特点;葡聚糖凝胶微柱离心法能有效分离游离药物和固体脂质纳米粒,所测得的包封率数据稳定差异小。结论本实验成功制备苦参碱固体脂质纳米粒,并对其粒径、电位和体外释放进行了质量评价;建立的葡聚糖凝胶微柱法为水溶性药物固体脂质纳米粒的包封率测定提供可靠参考。OBJECTIVE To prepare matrine solid lipoid nanoparticle,establish preparating method and determine the encapshlation efficiency.METHODS Matrine solid lipoid nanoparticle was prepared by microemulsion-probe ultrasonic method and its quality was evaluated by particle size,Zeta potential,microscopic morphology and in vitro release.The encapsulation efficiency of the carrier was measured by different methods and their effect was compared.RESULTS The diameter of matrine solid lipoid nanoparticle was(116.7±2.6)nm and its Zeta potential was(-45±1.7)mV.Transmission electron micrographs showed that the solid lipoid nanoparticle was uniform in size and spherical.The in vitro release result suggested the carrier exhibited control release character.Dextran gel microcolumn centrifugation can effectively separate free drugs and carriers,and the measured encapsulation efficiency data has little difference in stability.CONCLUSION Matrine solid lipoid nanoparticle is successfully prepared and their particle size,Zeta potential and in vitro release quality are evaluated.Dextran gel microcolumn method is effective in the measurement of matrine solid lipoid nanoparticle,providing a reliable reference for the determination of water-soluble drug encapsulation efficiency.

关 键 词：苦参碱 固体脂质纳米粒 包封率 

分 类 号：R944[医药卫生—药剂学]