目的 研究电穿孔技术对小分子离子型药物经皮渗透的影响。方法 以盐酸丁卡因为小分子离子型模型药物，使用双室扩散池方法研究电穿孔对其在离体大鼠腹部皮肤经皮渗透的影响，并与被动扩散和离子导入进行比较。结果 外加电脉冲（方波脉冲，脉冲幅度为130 V，脉冲宽度为 0.4 s，脉冲率为40 pulses·min-1）后，盐酸丁卡因的渗透速率较被动扩散增加3.5倍以上，比离子导入（0.2 mA·cm-2，4 h）增加1倍以上；并且渗透速率随着脉冲数的增加而增加。结论 电穿孔技术能明显地促进小分子离子型药物盐酸丁卡因的经皮渗透。
Abstract
OBJECTIVE To study the effects of electroporation on the permeation of small molecular ion drug through skin in vitro. METHODS Using valia-chien two-chamber diffusion cells,the fluxes of tetracaine hydrochloride achieved with passive diffusion,electroporative pulse and iontophoresis were compared. RESULTS The application of electroporative pulse or iontophoresis increased the permeation of tetracaine hydrochloride.The flux of tetracaine hydrochloride with electroporative pulse (square wave pulse,voltage=130 V,pulse time=0.4 s,pulse freqency=40 pulses·min-1) was 4 times or 2 times higher than that of passive diffusion or iontophoresis (0.2 mA·cm-2,4 h),respectively.When the pulse number was increased,the flux of tetracaine hydrochloride was increased. CONCLUSION The permeation of tetracaine hydrochloride through skin can be increased by electroporation.
关键词
电穿孔 /
经皮渗透 /
盐酸丁卡因 /
离子导入
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Key words
electroporation /
transdermal delivery /
tetracaine hydrochloride /
iontophoresis
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参考文献
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脚注
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基金
国家自然科学基金资助项目(39670857)
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