以茶皂素为天然乳化剂制备水飞蓟素纳米乳及其理化性质考察  

Preparation of silymarin nanoemulsion with tea saponins as natural emulsifiers and investigation of its physicochemical property

作　　者：邓茂 李小芳[1] 陈慧娟 谢龙 张旭敏 刘凯 DENG Mao;LI Xiao-fang;CHEN Hui-juan;XIE Long;ZHANG Xu-min;LIU Kai(Key Laboratory of Standardization of Chinese Herbal Medicine,Ministry of Education,Key Laboratory of Systematic Research,Development and Utilization of Chinese Medicine Resources in Sichuan Province,Key Laboratory Breeding Base of Co-founded by Sichuan Province and Ministry of Science and Technology,College of Pharmacy,Chengdu University of Traditional Chinese Medicine,Chengdu 611137,China)

机构地区：[1]成都中医药大学药学院,中药材标准化教育部重点实验室,四川省中药资源系统研究与开发利用重点实验室-省部共建国家重点实验室培育基地,四川成都611137

出　　处：《中草药》2021年第21期6528-6536,共9页Chinese Traditional and Herbal Drugs

基　　金：四川省科技厅项目(2019YFS0113);四川省科技厅项目(2020095)。

摘　　要：目的以茶皂素为天然乳化剂制备水飞蓟素纳米乳(silymarin nanoemulsion,SM-NE)。方法使用高速剪切联合高压均质法制备SM-NE,以平均粒径、粒度多分散系数(polydispersity index,PDI)、分层指数和外观为主要评价指标,采用单因素试验对处方和制备工艺进行优化;以摩尔增溶比(molar solubilization ratio,MSR)和胶束-水分配系数(Km)作为评价指标探究了茶皂素对水飞蓟素的增溶能力;对最佳处方和工艺制备的SM-NE进行了理化性质和稳定性考察。结果SM-NE的最佳处方为水飞蓟素用量0.15%,茶皂素用量为0.3%,油相用量为5%,最佳制备工艺为剪切速率16000 r/min,剪切时间3 min,均质压力为100 MPa,均质次数为8次;茶皂素对水飞蓟素增溶参数值MSR和Km分别为0.0111和2.31;制得的SM-NE的平均粒径为(204.1±2.8)nm,PDI为0.058±0.007,电导率为(117.8±0.9)μs/cm,pH值为7.31±0.10,浊度为(59.75±1.10)cm^(−1),水飞蓟素溶解度为(1.22±0.05)mg/mL;稳定性结果显示,SM-NE具有良好的离心稳定性和储存稳定性。结论以茶皂素为天然乳化剂成功制备了稳定的SM-NE,茶皂素是一种潜在的用于水飞蓟素新型绿色纳米制剂生产的天然增溶剂。Objective The tea saponins(TS)were used as a natural emulsifier to prepare silymarin nanoemulsion(SM-NE).Methods The SM-NE was prepared by high-speed shear combined with high-pressure homogenization.The particle size,polydispersity index(PDI),delamination index and appearance were the main evaluation indicators.The optimal prescription and process parameters were screened out by single factor test;Molar solubilization ratio(MSR)and micelle-water partition coefficient(Km)were used as evaluation indexes to explore the solubilization ability of TS to silymarin.The physicochemical property and stability of the SM-NE prepared by the optimal prescription and process parameters were studied.Results The best prescription of SM-NE was 0.15%of silymarin,0.3%of TS,and 5%of oil phase.The shear rate and time were 16000 r/min and 3 min,the homogenization pressure and times were 100 MPa and 8.The solubilization parameters MSR and Km of TS to silymarin were 0.0111 and 2.31 respectively.The mean particle size of the prepared SM-NE was(204.1±2.8)nm,PDI was 0.058±0.007,conductivity was(117.8±0.9)μs/cm,pH was 7.31±0.10,turbidity was(59.75±1.10)cm^(−1),and solubility of silymarin was(1.22±0.05)mg/mL.The stability results showed SM-NE had good centrifugal stability and storage stability.Conclusion Using TS as the natural emulsifier,the stable SM-NE was successfully prepared.TS is a potential natural solubilizer for the production of n new green nano-pharmaceutics of silymarin.

关 键 词：纳米乳 茶皂素 水飞蓟素 理化性质 增溶 高速剪切联合高压均质法 

分 类 号：R283.6[医药卫生—中药学]