超声波导入的促渗作用及其对皮肤微观结构的影响

Sonophoresis Induces the Enhanced Permeation of Drug and Its Effect on Stratum Corneum

关键词:  超声波导入  经皮渗透  氢溴酸高乌甲素  凝胶  角质层

Key words:  sonophoresis  transdermal permeation  lappaconitine hydrobromide  gel  stratum corneum

摘要:

目的考察超声波导入对高乌甲素水凝胶经皮渗透的促进作用及其对皮肤角质层微细结构的影响。方法制备了高乌甲素卡波姆凝胶，分别采用频率为800 kHz和1 MHz的超声波在体外进行了经鼠皮渗透实验，定时测定接受室药物浓度并计算经皮渗透参数。制备皮肤切片，分别采用光镜和扫描电镜观察皮肤及角质层微细结构的改变。结果800 kHz和1 MHz的超声波导入对高乌甲素稳态透皮速率的促渗倍数分别达到约7倍和23倍。角质层微细结构观察发现超声波引起了皮肤表面空隙的增加和结构的改变。结论超声波导入显著促进了高乌甲素的经皮渗透，并提示空化效应是引起促渗作用的重要因素。

Abstract:

OBJECTIVE To investigate the effect of sonophoresis on both the transdermal permeation of lappaconitine hydrobromide and the micro-structure of stratum corneum. METHODS Drug-containing gel composed of carbomer 934 was prepared. In vitro transcutaneous delivery of lappaconitine hydrobromide with or without sonophoresis which frequencies were 800 kHz and 1 MKz, respectively, were carried out using rat skin and modified Franz diffusion cells. Drug concentration in receive cell was determined at scheduled intervals and the permeation parameters were calculated. The change of skin and stratum corneum after the treatment of sonophoresis was observed by both normal microscope and scanning electric microscope. RESULTS Sonophoresis at frequencies of 800 kHz and 1 MHz induced the enhancing rate of drug permeated to about 7-fold and 23-fold, respectively, compared to that of passive diffusion. The surface of stratum corneum was changed by the ultrasound. CONCLUSION Sonophoresis can enhance the transdermal permeation of lappaconitine hydrobromide notably and which was probable via the cavitation effect.