细辛挥发油促进芥子碱经皮渗透及其促透机制研究
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摘要
目的研究细辛Asari Radix et Rhizoma挥发油促进芥子碱经皮渗透及其机制。方法首先采用经皮水分丢失仪测定细辛挥发油作用后皮肤经皮水分丢失的变化,以此来确定细辛挥发油作用皮肤后是否降低皮肤屏障功能。然后以SD大鼠背部皮肤作为渗透屏障,利用扩散池法研究细辛挥发油对芥子碱的体外经皮累积渗透量及皮肤滞留量的影响;并通过SD大鼠在体经皮给药测定给药24 h后皮肤中芥子碱透过量,进一步验证细辛挥发油对芥子碱的促渗作用。随后,利用全反射傅里叶红外变换光谱(ATR-FTIR)和差示扫描量热法(DSC)表征细辛挥发油作用后大鼠皮肤角质层中脂质和蛋白变化,观察细辛挥发油对大鼠皮肤角质层脂质和蛋白的影响。结果皮肤经皮水分丢失率(TEWL)测定结果表明,细辛挥发油作用于大鼠皮肤后,TEWL值升高,皮肤屏障功能降低。离体透皮实验结果表明含细辛挥发油组的芥子碱的经皮累积渗透量及皮肤滞留量都明显高于不含细辛挥发油组;在体透皮实验进一步验证了细辛挥发油促进芥子碱在皮肤的滞留。ATR-FTIR和DSC结果表明,与细辛挥发油未作用组相比,细辛挥发油作用后皮肤角质层中的脂质和角蛋白构象发生紊乱,皮肤的渗透性增加。结论细辛挥发油可促进芥子碱的经皮渗透,其促透机制与细辛挥发油紊乱皮肤角质脂质和蛋白的流动性相关。
Objective To study the enhancing effect of essential oil from asarum(EOA) on percutaneous delivery of sinapine and its mechanism. Methods Transepidermal water loss(TEWL) was determined with Vapo Meter to evaluate the decrease of skin barrier by asarum essential oil. In vitro permeation of sinapine through rat skin was performed in the presence or absence of EOA, and the permeated cumulative amount and retention of sinapine were compared. In vivo percutaneous test was further performed to estimate the improvement of EOA on percutaneous delivery of sinapine. Attenuated total reflection Fourier transform infrared spectroscopy(ATR-FTIR) and differential scanning calorimeter(DSC) were used to evaluate the changes of lipid and protein in stratum corneum. Results TEWL value increased after the treatment of EOA, which indicated the decrease of skin barrier. The permeated cumulative amount and retention of sinapine in the presence of EOA were higher than those in the absence of EOA, and in vivo percutaneous test further confirmed this issue. After EOA treatment, the lipid and protein disorder could be observed from ATR-FTIR and DSC map, which indicated the increasing of skin permeability. Conclusion EOA can enhance the percutaneous delivery of sinapine through improving the disorder of lipid and protein of stratum corneum.
Objective To study the enhancing effect of essential oil from asarum(EOA) on percutaneous delivery of sinapine and its mechanism. Methods Transepidermal water loss(TEWL) was determined with Vapo Meter to evaluate the decrease of skin barrier by asarum essential oil. In vitro permeation of sinapine through rat skin was performed in the presence or absence of EOA, and the permeated cumulative amount and retention of sinapine were compared. In vivo percutaneous test was further performed to estimate the improvement of EOA on percutaneous delivery of sinapine. Attenuated total reflection Fourier transform infrared spectroscopy(ATR-FTIR) and differential scanning calorimeter(DSC) were used to evaluate the changes of lipid and protein in stratum corneum. Results TEWL value increased after the treatment of EOA, which indicated the decrease of skin barrier. The permeated cumulative amount and retention of sinapine in the presence of EOA were higher than those in the absence of EOA, and in vivo percutaneous test further confirmed this issue. After EOA treatment, the lipid and protein disorder could be observed from ATR-FTIR and DSC map, which indicated the increasing of skin permeability. Conclusion EOA can enhance the percutaneous delivery of sinapine through improving the disorder of lipid and protein of stratum corneum.
引文
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[2]李磊,张涛,张小梅.三伏贴在肺系疾病中的应用进展[J].针灸临床杂志,2012,28(6):87-88.
[3]郭秀彩,刘霞,徐月红.白芥子涂方穴位与非穴位给药皮肤渗透特性的比较研究[J].中国中药杂志,2012,37(7):1034-1038.
[4]刘霞,郭秀彩,林媛媛,等.穴位与非穴位皮肤生物物理学性质影响芥子碱渗透特性研究[J].中草药,2013,44(9):1111-1116.
[5]徐月红,叶卉,官素桃,等.穴白芥子涂方凝胶膏剂的体外释放及透皮特性研究[J].中成药,2011,33(12):2068-2072.
[6]程欣,马云淑,阎红,等.细辛挥发油对大黄藤素体外促透皮作用的实验研究[J].云南中医学院学报,2008,31(2):15-19.
[7]程欣,马云淑,阎红,等.细辛挥发油对颅痛定的裸鼠体外促透的作用[J].华西药学杂志,2008,23(1):4-6.
[8]黎丽,闫小平,郑蕊,等.新型伤湿止痛贴膏剂体外释药规律研究[J].中草药,2011,42(12):2430-2433.
[9]陈军,刘培,蒋秋冬,等.中药挥发油作为透皮吸收促进剂的现状与展望[J].中草药,2014,45(24):3561-3565.
[10]吴建兵,褚襄平,张永煜,等.五味子-细辛药对抗哮喘活性部位筛选[J].中华中医药学刊,2013,31(1):121-123.
[11]中国药典[S].一部.2015.
[12]薛漫清,梁庆,黄钊,等.利用ATR-FTIR变化探讨薄荷醇对皮肤角质层结构的影响[J].中草药,2012,43(12):2474-2477.
[13]Schwarz J C,Pagitsch E,Valenta C.Comparison of ATRFTIR spectra of porcine vaginal and buccal mucosa with ear skin and penetration analysis of drug and vehicle components into pig ear[J].Eur J Pharm Sci,2013,50(5):595-600.
[14]Glassford S E,Byrne B,Kazarian S.Recent applications of ATR FTIR spectroscopy and imaging to proteins[J].Biochim Biophys Acta,2013,1834(12):2849-2858.
[15]赵茜,李伟泽,程玉钏,等.几种挥发油对黄藤素透皮给药的促渗作用研究[J].应用化工,2016,45(1):186-189.