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13000r/min、剪切时间2min、均质压力100MPa、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)m V、溶解度(460.3±2.1)μg/m L、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。
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.
引文
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