目的 研究甘草次酸-壳聚糖纳米粒(GA-CS-NPs)的最佳制备处方并对其进行质量评价。方法 采用离子交联法制备GA-CS-NPs, 以粒径、载药量、包封率为综合评价指标, 通过单因素、正交设计试验优化制备工艺及处方, 通过形态观察、粒径、载药量及包封率的考察对其进行质量评价。结果 最佳处方组合为甘草次酸(GA)质量浓度为0.2 mg/mL, 壳聚糖(CS)质量浓度为2 mg/mL, CS溶液与三聚磷酸钠(TPP)溶液(1.0 mg/mL)的体积比为20:3, 所制备的GA-CS-NPs平均粒径(310.27±10.02)nm, 包封率(51.42±0.43)%, 载药量(6.87±0.47)%。质量评价结果表明, GA-CS-NPs外观圆整、均匀, 在低温条件下, 具有一定的稳定性。结论 离子交联法制备GA-CS-NPs工艺简单、可靠, 产品稳定性好。

Objective To study the optimal preparation process of glycyrrhetinic acid-chitosan nanoparticles (GA-CS-NPs) and to evaluate the quality. Methods The GA-CS-NPs were prepared by ionic cross-linking. The particle size, drug loading, and encapsulation efficiency were as evaluation indexes. The prescription and preparation process were optimized through single factor and orthogonal design. The quality of GA-CS-NPs was evaluated by morphology, particle size, drug loading, and encapsulation efficiency. Results The optimal prescription was as follows: concentration of GA and CS was 0.2 and 2 mg/mL, ratio of CS and TPP (1.0 mg/mL) solutions was 20:3. The mean diameter of GA-CS-NPs was (310.27 ± 10.02) nm, the entrapment efficiency and drug-loading efficiency were (51.42 ± 0.43)% and (6.87 ± 0.47)%. The evaluation showed that the appearance of GA-CS-NPs was round and uniform. It had a certain stability under lower temperature. Conclusion The ionic cross-linking method used to prepare GA-CS-NPs is simple, rational, and stable.

甘肃省科技支撑计划—甘草次酸口服囊泡包裹的纳米载体构建及肝靶向特性研究(1204FKCA183)