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引用本文:朱聪聪,喻琴,潘会君,陈亚,缪晓,朱全刚.青蒿精油作为纳米乳油相促进雷公藤红素透皮吸收的研究[J].中国现代应用药学,2022,39(8):1054-1058.
ZHU Congcong,YU Qin,PAN Huijun,CHEN Ya,MIAO Xiao,ZHU Quangang.Effect of Artemisia Oil in the Nanoemulsion as an Oil Excipient and Enhancer on Percutaneous Absorption of Celastrol[J].Chin J Mod Appl Pharm(中国现代应用药学),2022,39(8):1054-1058.
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青蒿精油作为纳米乳油相促进雷公藤红素透皮吸收的研究
朱聪聪1,2, 喻琴1,2, 潘会君1,2, 陈亚1,2, 缪晓3, 朱全刚1,2
1.上海市皮肤病医院, 上海 200443;2.上海中药外用制剂创新工程技术研究中心, 上海 200443;3.上海中医药大学创新中药研究院, 上海 201203
摘要:
目的 探究青蒿精油及其纳米乳对雷公藤红素体外透皮吸收的影响及促透机制。方法 首先建立雷公藤红素含量测定方法,其次制备以青蒿精油作为油相的纳米乳并表征,最后采用改良Franz扩散池法考察不同浓度青蒿精油及以青蒿精油作为纳米乳油相对雷公藤红素的促透效果,并用HE染色、差示扫描量热法探究促透机制。结果 雷公藤红素浓度在1.8~360 μg·mL-1内线性关系良好,线性回归方程Y=16 494X–16 111(r=1.000);精密度、稳定性的RSD<2%,平均加样回收率为99.26%,RSD为1.04%。雷公藤红素纳米乳平均粒径(19.93±0.19)nm,Zeta电位为(17.67±2.78)mV,多分散性指数为0.097。纳米乳、青蒿精油及含青蒿精油的纳米乳对雷公藤红素均有不同程度的促渗作用,对皮肤结构、相变温度均有不同程度改变。其中,含青蒿精油的纳米乳对雷公藤红素的促渗作用最强、对皮肤结构和相变温度影响最大。结论 青蒿精油及以青蒿精油作为纳米乳油相对雷公藤红素具有较好的促透作用,其促透机制与影响皮肤结构、改变热力学性质有关。
关键词:  雷公藤红素  青蒿精油  纳米乳  透皮吸收
DOI:10.13748/j.cnki.issn1007-7693.2022.08.008
分类号:R943
基金项目:上海市“科技创新行动计划”项目(21S21900900,20DZ2255200)
Effect of Artemisia Oil in the Nanoemulsion as an Oil Excipient and Enhancer on Percutaneous Absorption of Celastrol
ZHU Congcong1,2, YU Qin1,2, PAN Huijun1,2, CHEN Ya1,2, MIAO Xiao3, ZHU Quangang1,2
1.Shanghai Skin Disease Hospital, Shanghai 200443, China;2.Shanghai Engineering Research Center for Topical Chinese Medicine, Shanghai 200443, China;3.Innovation Research Institute of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China
Abstract:
OBJECTIVE To explore the effects and mechanism of artemisia oil and its nanoemulsion on transdermal absorption in vitro of celastrol. METHODS Firstly, the method for determination of celastrol content was established. Then, the nanoemulsion with artemisia oil as the oil phase was prepared and characterized. Finally, transdermal tests were performed by improved Franz diffusion cells in order to investigate the effect of different concentrations of artemisia oil and its nanoemulsion on the transdermal penetration of celastrol. HE staining and differential scanning calorimetry were applied to evaluate the skin stratum corneum changes. RESULTS The method for determination of celastrol content had a good linear relationship in the detection range of 1.8-360 μg·mL-1, and the linear regression equation was Y=16 494X-16 111(r=1.000). The RSDs of precision and stability were <2%. The average recovery of celastrol was 99.26%, RSD was 1.04%. The average diameter of celastrol nanoemulsion was (19.93±0.19)nm, Zeta potential was (17.67±2.78)mV and the polydispersity index was 0.097. Nanoemulsion(not containing artemisia oil), artemisia oil and its microemulsion could enhance the transdermal permeability of celastrol and change the skin structure and temperature to different degrees, but the effects varied. Among them, microemulsion containing artemisia oil was the optimum option to improve the percutaneous absorption of celastrol at a highest level. CONCLUSION Artemisia oil has a good penetration-promoting effect on celastrol, and its penetration-promoting mechanism is related to affecting the structure of the skin and changing the thermodynamic properties.
Key words:  celastrol  artemisia oil  nanoemulsion  transdermal absorption
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