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 mL,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 within 24 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 mL). 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.

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