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

Effect of Artemisia Oil in the Nanoemulsion as an Oil Excipient and Enhancer on Percutaneous Absorption of Celastrol

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1.8~360μg·mL^(−1)内线性关系良好,线性回归方程Y=16494X-16111(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。

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 1.8−360μg·mL^(−1),and the linear regression equation was Y=16494X−16111(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.