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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 nanoparticles (Pae-LLCN) and investigate its in vitro release characteristics. Methods Pae-LLCN was prepared by spontaneous emulsification-sonication with the entrapment efficiency as an indicator. The prescription of Pae-LLCN was optimized by orthogonal design. The cumulative release of Pae-LLCN in 24 h was determined by dialysis method and plotted Drug release curve, using transmission electron microscopy, nanoparticle size instrument to examine its morphology and particle size. Results The optimal formulation of Pae-LLCN was poloxamer 407 (F127) and glycerol monooleate (GMO) 1:10, the dosage of paeoniflorin 40 mg and the amount of phosphate buffered saline (PBS) The average entrapment efficiency of the drug was 73.72% with drug loading of 14.81% and particle size of (170 ± 16) nm. The cumulative release in 24 h was 72.68%. Conclusion Pae-LLCN preparation is reasonable and feasible, good stability, with good sustained-release effect.