[关键词]
[摘要]
目的 制备以甘草酸作为乳化剂的橙皮苷纳米乳液(HDN-NE),以期开发橙皮苷的新型绿色纳米制剂。方法 采用高速剪切-高压均质技术制备HDN-NE,以粒径、PDI、外观为主要评价指标筛选处方工艺,对以最佳处方工艺制备的HDN-NE的理化性质和相关稳定性进行研究。结果 HDN-NE的最佳制备处方为橙皮苷用量0.1%、甘草酸用量0.3%、油相用量5%,最佳工艺参数为剪切速率13 000 r/min、剪切时间2 min、均质压力100 MPa、均质次数6次;制得纳米乳平均粒径为(262.7±3.1)nm、PDI为0.234±0.009、Zeta电位为(-35.42±0.72)mV、溶解度(460.3±2.1)μg/mL、电导率(116.4±1.7)μs/cm、pH值为6.820±0.008、浊度为451 cm-1(n=3);经染色法鉴别为O/W乳液,透射电镜观察乳滴呈圆球状,大小均一;稳定性研究结果表明HDN-NE稳定性良好。结论 以甘草酸作为乳化剂的HDN-NE可显著提高橙皮苷的溶解度及稳定性,是一种潜在的安全性高的新型纳米药物。
[Key word]
[Abstract]
Objective To prepare a new hesperidin nanoemulsion (HDN-NE) with glycyrrhizic acid as emulsifier, by which could develop a "new green nano-pharmaceutics" of hesperidin. Methods HDN-NE was prepared by high-speed shearing and high-pressure homogenization. The prescription of HDN-NE was optimized with particle size, PDI, and appearance as indexes. The physicochemical property and stability of HDN-NE prepared by the optimal prescription were studied. Results The optimal prescription of HDN-NE was as follow:The content of hesperidin, glycyrrhizic acid, and oil phase were 0.1%, 0.3%, and 5%, respectively. The shear rate was 13 000 r/min, the cutting time was 2 min, the homogeneous pressure and times were 100 MPa and 6, severally. The result showed that the prepared HDN-NE had the mean size of (262.7 ±3.1) nm, PDI of 0.234 ±0.009, Zeta potential of (−35.42 ±0.72) mV, and solubility of (460.3 ±2.1) μg/mL. The physicochemical property study showed that the conductivity was (116.4 ±1.7) μs/cm, the pH was 6.820 ±0.008, and the turbidity was 451 cm−1 (n=3). It was identified as O/W emulsion by dyeing method. The droplets were spherical and uniform by transmission electron microscopy. The stability study showed that HDN-NE had good stability. Conclusion HDN-NE with glycyrrhizic acid as an emulsifier can significantly improve the solubility and stability of hesperidin, which is a new potential nano-drug with safety.
[中图分类号]
R283.6
[基金项目]
四川省中医药管理局科技项目(2018YY001)