茶皂素稳定的芹菜素纳米乳制备及其体外释放研究  

Preparation and in vitro release of tea saponin-stabilized apigenin nanoemulsion

作　　者：张旭敏 谢龙 赵雨芯 李芝蓓 李小芳[1] ZHANG Xu-min;XIE Long;ZHAO Yu-xin;LI Zhi-bei;LI Xiao-fang(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》2022年第17期5348-5355,共8页Chinese Traditional and Herbal Drugs

基　　金：四川省科技厅科研项目(CN)(2020095);四川省科技厅科研项目(2019YFS0113)。

摘　　要：目的 以茶皂素为天然乳化剂制备芹菜素纳米乳液(AP-NE),并对其进行稳定性和体外释放特性的考察,以期获得新型绿色的纳米制剂。方法 采用高速剪切结合高压均质技术制备AP-NE,以平均粒径和多分散指数(PDI)为自变量,运用总评归一值(OD)法对数据进行处理,采用Box-Behnken效应面法优化处方并进行验证,并对最优处方制备的AP-NE进行理化性质和体外释放特性考察。结果 优化结果表明AP-NE的最优制备处方为芹菜素质量分数0.40%、茶皂素质量浓度2.0 mg/mL、油相用量(蓖麻油-辛癸酸甘油酯1∶3)3 mL;测得AP-NE的平均粒径为(259.5±3.6)nm、PDI为0.103±0.005、ζ电位为(-35.81±0.42)mV、电导率为(88.60±1.00)μS/cm,pH为7.37±0.08,溶解度为(128.12±1.35)μg/mL,载药量为(5.77±0.08)%,浊度为(99.45±1.69)cm^(-1)(n=3);经染色法鉴别为O/W乳液,透射电子显微镜观察乳滴不粘连,大小均一,呈圆球状;稳定性试验表明AP-NE稳定性良好;体外释放研究表明AP-NE中芹菜素的释放具有缓慢和持续的趋势。结论 以茶皂素作为乳化剂制备的纳米乳可明显提高芹菜素的溶解度和稳定性,是一种潜在的可提高药物有效性的新型纳米制剂。Objective To prepare apigenin nanoemulsion(AP-NE) with tea saponin as natural emulsifier, and investigate its stability and release characteristics in vitro, in order to obtain a new green nano-formulation. Methods AP-NE was prepared by high-speed shearing combined with high-pressure homogenization technology. The average particle size and polydispersity index(PDI) were used as independent variables, and the data were processed by the overall desirability value(OD) method. The formulation was optimized and verified by Box-Behnken effect surface method, and the physicochemical properties and in vitro release characteristics of AP-NE prepared with the optimal formulation were investigated. Results The optimal prescription of AP-NE was as follows:apigenin at a concentration of 0.40%, tea saponin at a concentration of 2.0 mg/mL, oil phase(castor oil: caprylic capric triglyceride=1:3) in an amount of 3 mL;The measured average particle size of AP-NE was(259.5 ± 3.6) nm, PDI was 0.103 ± 0.005, ζ potential was(-35.81 ± 0.42) mV, conductivity was(88.60 ± 1.00) μS/cm, and pH was 7.37 ± 0.08, solubility was(128.12 ± 1.35) μg/mL,drug loading was(5.77 ± 0.08)%, turbidity was(99.45 ± 1.69) cm^(-1)(n = 3);it was identified as O/W emulsion by staining method,TEM observed that the milk droplets were non-adherent, uniform in size and spherical;stability test showed that AP-NE had good stability;in vitro release study showed that the release of apigenin from AP-NE had a slow and continuous trend. Conclusion Nanoemulsion prepared with tea saponin as emulsifier can greatly improve the solubility and stability of apigenin, and it is a potential new nano-formulation that can improve drug effectiveness.

关 键 词：芹菜素 纳米乳 茶皂素 高速剪切-高压均质技术 BOX-BEHNKEN效应面法 理化性质 稳定性 体外释放 

分 类 号：R283.6[医药卫生—中药学]