基于“药辅合一”理念的当归精油纳米乳递药系统的构建、表征及评价  

Construction,characterization and evaluation of Angelica Sinensis Radix essential oil-loaded nanoemulsion drug delivery system based on concept of“combination of drugs and adjuvants”

作　　者：邱菁 徐纯艺 周玮玲 赵淋仙 李燕燕 胡慧玲[1] QIU Jing;XU Chun-yi;ZHOU Wei-ling;ZHAO Lin-xian;LI Yan-yan;HU Hui-ling(State Key Laboratory of Southwestern Traditional Chinese Medicine Resources,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,西南特色中药资源国家重点实验室,四川成都611137

出　　处：《中草药》2023年第6期1783-1792,共10页Chinese Traditional and Herbal Drugs

基　　金：四川省科技厅项目(2019ZYZF0171)。

摘　　要：目的构建当归精油纳米乳(Angelica Sinensis Radix essential oil-loaded nanoemulsion,AEO-NE)递药系统并对其进行表征及稳定性、毛囊靶向、毛发生长促进作用评价。方法分别应用伪三元相图法和星点设计-响应面法(central composite experiment design-response surface method,CCD-RSM)对纳米乳处方进行筛选和优化。对纳米乳乳剂类型、粒径、ζ电位、多分散指数(polydispersity index,PDI)、微观形态、黏度、pH值进行表征。以粒径、PDI、外观变化及Z-藁本内酯含量为指标,评价最优处方纳米乳离心稳定性、放置稳定性以及稀释稳定性。通过在体给药荧光标记的AEO-NE于小鼠背部皮肤研究制剂毛囊靶向能力。应用C57BL/6小鼠研究AEO-NE体内促进毛发生长的作用。结果AEO-NE最优处方为AEO-辛基酚聚氧乙烯醚10(OP-10)-无水乙醇-水(2.25∶0.75∶1∶96);按最优处方所制AEO-NE外观澄清、透明、微泛蓝光,乳剂类型为O/W型,平均粒径为(15.95±0.33)nm,PDI为0.11±0.02,ζ电位为(-0.14±0.10)m V,pH值为5.89±0.16,黏度为(1.57±0.08)m Pa·s,透射电镜结果表明AEO-NE乳滴呈球形,外观圆整,大小在20 nm内。AEO-NE离心稳定性、稀释稳定性良好,在4℃条件下密封避光放置稳定性良好,粒径及Z-藁本内酯含量无显著变化。AEO-NE局部皮肤给药24 h内均表现出毛囊靶向性,具有促进毛发生长的作用。结论基于“药辅合一”理念,成功构建了以AEO为唯一油相的AEONE,其宏观及微观形态、相关理化性质符合纳米乳制剂要求,稳定性良好,在靶向促进毛发生长方面具有一定潜力。Objective To prepare,characterize Angelica Sinensis Radix essential oil(AEO)-loaded nanoemulsion(AEO-NE)and evaluate on its hair follicle targeted capacity,hair growth promoting effect and stability.Methods The pseudo-ternary phase diagram method and central composite design-response surface method(CCD-RSM)were used to screen and optimize the prescription of AEONE,respectively.The type,average droplet size,ζpotential,polydispersion index(PDI),microscopic morphology,viscosity and pH of AEO-NE were characterized.The centrifugation stability,placement stability and dilution stability of the optimized AEO-NE were evaluated with particle size,PDI,appearance change and content of Z-ligustilide as indicators.The hair follicle targeted ability of AEONE was investigated by administrating fluorescin-labeled AEO-NE to the back skin of mice in vivo.The promoting effect of AEO-NE on hair growth was studied in C57BL/6 mice.Results The optimized formula of AEO-NE consisted 2.25%octylphenol polyoxyethylene ether 10(OP-10),0.75%absolute ethanol,1%AEO and 96%water;The appearance of the optimized AEO-NE was clear,transparent and slightly blue.The emulsion type is O/W type,the average particle size was(15.95±0.33)nm,the PDI was 0.11±0.02,theζpotential was(-0.14±0.10)mV,the pH value was 5.89±0.16,and the viscosity was(1.57±0.08)mPa·s.The result of transmission electron microscope showed that AEO-NE was spherical and round,and its size was within 20 nm.AEO-NE had good stability in centrifugation and dilution,and was stable at 4℃avoiding light with no significant changes in droplet size and Z-ligustilide content.AEO-NE showed hair follicle targeted property within 24 h with local skin administration,and had the effect of promoting hair growth.Conclusion Based on the concept of“combination of drugs and adjuvants”,the AEO-NE with AEO as the only oil phase was successfully constructed.Its macro-and micro-morphology,related physical and chemical properties met the requirements of nanoemulsion preparation.With good stability,A

关 键 词：当归精油 纳米乳 伪三元相图 星点设计-响应面法 表征 稳定性评价 毛囊靶向 促进毛发生长 

分 类 号：R283.6[医药卫生—中药学]