Gujjar Meera, Banga Ajay K
College of Pharmacy, Mercer University, Atlanta, GA 30341, USA.
College of Pharmacy, Mercer University, Atlanta, GA 30341, USA.
Int J Pharm. 2014 Sep 10;472(1-2):362-8. doi: 10.1016/j.ijpharm.2014.06.050. Epub 2014 Jun 27.
The purpose of this study was to compare the transdermal permeation of a model compound, diclofenac diethylamine, from a hydrophilic and lipophilic vehicle across in vitro models simulating compromised skin. Mineral oil served as a lipophilic vehicle while 10mM phosphate buffered saline served as a hydrophilic vehicle. Compromised skin was simulated by tape stripping, delipidization, or microneedle application and compared with intact skin as a control. Transepidermal water loss was measured to assess barrier function. Skin compromised with tape stripping and delipidization significantly (p<0.05) increased permeation of diclofenac diethylamine compared to intact and microneedle treated skin with phosphate buffered saline vehicle. A similar trend in permeation was observed with mineral oil as the vehicle. For both vehicles, permeation across skin increased in the same order and correlated with degree of barrier impairment as indicated by transepidermal water loss values: intact<microneedles<tape stripping<delipidization. A study with hairless rats comparing both vehicles found the same trend, with hydrophilic vehicle having greater delivery. In conclusion, phosphate buffered saline vehicle resulted in higher permeation into and across skin compared to mineral oil vehicle for all simulated models of compromised skin.
本研究的目的是比较模型化合物双氯芬酸二乙胺在亲水性和疏水性载体中通过模拟受损皮肤的体外模型的透皮渗透情况。矿物油作为疏水性载体,而10mM磷酸盐缓冲盐水作为亲水性载体。通过胶带剥离、脱脂或微针应用模拟受损皮肤,并与完整皮肤作为对照进行比较。测量经表皮水分流失以评估屏障功能。与使用磷酸盐缓冲盐水载体的完整皮肤和微针处理皮肤相比,经胶带剥离和脱脂处理的皮肤显著(p<0.05)增加了双氯芬酸二乙胺的渗透。以矿物油作为载体时观察到类似的渗透趋势。对于两种载体,皮肤的渗透以相同顺序增加,并与经表皮水分流失值所表明的屏障损伤程度相关:完整皮肤<微针处理皮肤<胶带剥离皮肤<脱脂皮肤。一项对无毛大鼠比较两种载体的研究发现了相同的趋势,亲水性载体具有更高的递送量。总之,对于所有模拟的受损皮肤模型,与矿物油载体相比,磷酸盐缓冲盐水载体导致更高的皮肤渗透和经皮渗透。