雷公藤红素醇质体的制备及体外透皮性能研究

摘要

Objective To prepare celastrol ethosomes and to observe the permeability characteristics of the ethosomes which act as the transdermal delivery carriers of celastrol in vitro. Methods Celastrol ethosomes were prepared by ethanol injection method, and then the encapsulation efficiency, particle size, polydispersity index ( PDI) and zeta potential of the ethosomes were analyzed. TP2A intelligent percutaneous penetration instrument was used to compare the skin penetration properties of celastrol ethosomes, celastrol solution and the mixture of blank ethosomes with celastrol solution. Results The prepared celastrol ethosomes were spherical, and the average particle size was (401.3 ± 5.5) nm, PDI was 0.21± 0.02, steady zeta potential was (-2.75 ± 0.1) mV, and average encapsulation efficiency was ( 80.6 ± 0.7) %. The amount of accumulative penetration of celastrol ethosomes at 48 h was 76.86 μg·cm -2 and the permeation rate was 1.640 9 μg·cm -2·h -1, which were significantly higher than the celastrol solution and the mixture of blank ethosomes with celastrol solution. Conclusion The prepared ethosomes have high encapsulation efficiency, uniform particle size and stable quality, and are beneficial to the transdermal absorption of celastrol.%【目的】制备雷公藤红素（Cel）醇质体，并考察醇质体作为雷公藤红素经皮给药载体的渗透特性。【方法】采用乙醇注入法制备雷公藤红素醇质体，并对其包封率、粒径、多分散指数（PDI）及Zeta电位进行分析；采用TP2A型智能透皮试验仪进行体外透皮试验，比较雷公藤红素醇质体、空白醇质体/Cel溶液和Cel溶液的透皮行为。【结果】此方法制备的雷公藤红素醇质体为类球形结构，平均粒径为（401.3±5.5） nm， PDI为（0.21±0.02）， Zeta电位为（－2.75±0.1） mV，平均包封率为（80.6±0.7）%；醇质体48 h的累积透过量76.86μg·cm-2，渗透速率为1.6409μg·cm-2·h-1，与空白醇质体/Cel溶液和Cel溶液比较，均有显著提高。【结论】雷公藤红素醇质体的包封率较高，粒径分布均匀，质量稳定，且可显著促进雷公藤红素的透皮吸收。