芍药苷脂质液晶纳米粒制备及体外释放研究  

Preparation of paeoniflorin lipid liquid crystalline nanoparticles and its in vitro release

作　　者：邱玲[1,2] 尹蓉莉[1] 申宝德[2] 张利红[2] 武娜[2] 郑娟[1,2] 韩晋[2] 袁海龙[2] 

机构地区：[1]成都中医药大学药学院,四川成都611137 [2]中国人民解放军第三O二医院,北京100039

出　　处：《中草药》2015年第23期3495-3499,共5页Chinese Traditional and Herbal Drugs

基　　金：国家新药创制重大专项(2011ZX09201-201-14,2012ZX09J12108-04C,2013ZX09J13109-06C)

摘　　要：目的制备芍药苷脂质液晶纳米粒(Pae-LLCN),并考察其体外释药特性。方法以包封率为指标,采用自发乳化-超声法制备Pae-LLCN,用正交试验设计对Pae-LLCN的处方进行优化,用透析法测定Pae-LLCN在24 h内的累积释放量并绘制释药曲线,采用透射电镜、纳米粒度仪对其形态和粒径进行考察。结果 Pae-LLCN最佳处方为泊洛沙姆407(F127)与甘油单油酸酯(GMO)质量比为1∶10、芍药苷投料量为40 mg、磷酸盐缓冲液(PBS)的用量为20 m L,药物的平均包封率达到73.72%,载药量为14.81%,粒径(170±16)nm,体外24 h累积释放量为72.68%。结论 Pae-LLCN制备合理可行,稳定性好,有良好的缓释作用。Objective To prepare paeoniflorin lipid liquid crystalline nanoparticles（Pae-LLCN）, and to study its in vitro release behavior. Methods Using encapsulation efficiency（EE） as index, the Pae-LLCN were prepared by spontaneous emulsification and ultrasonic method, and the prescription of Pae-LLCN was optimized by orthogonal design. The in vitro release of Pae-LLCN within24 h was measured by dialysis method, afterwards its morphology and particle size were studied by transmission electron microscope（TEM）. Results The optimal formulation was poloxamer-glycerol monooleate（1∶ 10）, paeoniflorin inventory（40 mg）, and PBS solution（20 m L）. The average EE was 73.72%, the average DL was 14.81%, the size of nanoparticles was（170 ± 16） nm, and the 24 h in vitro accumulative release rate was 72.68%. Conclusion The optimized process is rational and feasible, and the Pae-LLCN has good stability with better sustained release in vitro.

关 键 词：芍药苷 脂质液晶纳米粒 体外释放 包封率 自发乳化-超声法 正交设计 透析法 

分 类 号：R283.6[医药卫生—中药学]