高乌甲素聚乳酸纳米粒的制备及体外释药特性的研究  

Preparation of Lappaconitine-Loaded Nanoparticles with Polylactic Acid and Its Release Properties in Vitro

作　　者：马君义[1,2] 陈香玲[1] 亢俊瑞 康雪蕾 王中煜[1] 张继[1,2] 刘嘉欣[3] 

机构地区：[1]西北师范大学生命科学学院,兰州730070 [2]甘肃特色植物有效成分制品工程技术研究中心,兰州730070 [3]中山大学生命科学大学院,广州510275

出　　处：《中国药学杂志》2015年第7期613-618,共6页Chinese Pharmaceutical Journal

摘　　要：目的制备载高乌甲素(LA)的聚乳酸(PLA)纳米粒,考察其体外释药特性。方法以生物可降解聚乳酸为载体材料,以聚乙烯醇(PVA)为乳化剂,采用乳化-溶剂挥发法制备载高乌甲素的聚乳酸纳米粒(高乌甲素-聚乳酸NPs),以包封率和载药量为主要评价指标,通过正交设计实验优化其制备工艺;运用激光粒度仪测定其粒径;原子力显微镜观察其形貌;动态透析法考察其体外释药特性。结果优化工艺制备的高乌甲素聚乳酸纳米粒外观呈圆形或类圆形,平均粒径为(429±9.19)nm,高乌甲素的包封率和载药量分别为(86.34±2.15)%,(45.85±1.34)%。体外释药研究表明,纳米粒能够连续释药15 d。结论成功制备了高乌甲素的聚乳酸纳米粒,其包封率、载药量高,体外释药具有明显的缓释特征。OBJECTIVE To prepare lappaconitine（LA）-loaded polylactic acid（PLA） nanoparticles（LA / PLA NPs） and investigate its release properties in vitro.METHODS LA / PLA NPs were prepared by optimized emulsion-solvent evaporation method with biodegradable PLA as carrier material and polyvinyl alcohol（PVA） as emulsifier.The entrapment efficiency and drug loading rate of LA were used as the main evaluation indexes to optimize the preparation process by orthogonal design method.The mean particle size was measured by laser particle size analyzer; the morphology of LA / PLA NPs was observed by atomic force microscope; the in vitro release behavior was studied by dynamic dialysis.RESULTS The optimized LA / PLA NPs were spherical.The mean particle size was（429 ± 9.19） nm,the entrapment efficiency and drug loading rate were（86.34 ± 2.15） % and（45.85 ± 1.34） %,respectively.The in vitro release study showed that the LA / PLA NPs could provide a continuous release of LA for 15 d.CONCLUSION LA / PLA NPs with high entrapment efficiency and drug loading rate are prepared successfully,and show sustained release effect for LA in vitro.

关 键 词：高乌甲素 聚乳酸 纳米粒 乳化-溶剂挥发法 正交设计 

分 类 号：R944[医药卫生—药剂学]