INVITRO AND INVIVO ENHANCEMENT OF SKIN PERMEATION WITH OLEIC AND LAURIC ACIDS
INVITRO AND INVIVO ENHANCEMENT OF SKIN PERMEATION WITH OLEIC AND LAURIC ACIDS
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DOI：
10.1016/0378-5173(88)90252-9
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发表时间：
1988-12-01
影响因子：
5.8
通讯作者：
HADGRAFT, J
中科院分区：
文献类型：
--
作者：
GREEN, PG;GUY, RH;HADGRAFT, J
使用Franz扩散池研究了两种脂肪酸（油酸和月桂酸）对阳离子药物萘甲唑啉、中性咖啡因和阴离子模型药物水杨酸盐在离体人皮肤中转运的影响。油酸和月桂酸甘油酯均增加所有渗透剂的体外皮肤渗透。油/水分配数据和旋转扩散池测量，在脂肪酸的存在下，表明阳离子萘甲唑啉的增强通量可以占通过与酸的羧酸根阴离子的离子配对增加亲油性。咖啡因和水杨酸钠不能形成离子对，因此，皮肤渗透性的增加也是由于角质层的破坏。这一结论进一步得到以下结果的支持：（a）经皮水分损失增加，和（B）在用脂肪酸预处理的皮肤部位，非离子配对烟酸甲酯的体内皮肤渗透增加。
The effect of two fatty acids (oleic and lauric) on the transport of the cationic drug naphazoline, neutral caffeine, and an anionic model drug salicylate, across excised human skin was studied using Franz diffusion cells. Oleic and lauric acis both increased the in vitro skin permeation of all penetrates. Oil/water partitioning data and rotating diffusion cell measurements, in the presence of the fatty acids, suggested that the enhanced flux of the cationic naphazoline could be accounted for by an increase in lipophilicity through ion pairing with the carboxylate anion of the acid. Caffeine and sodium salicylate were incapable of forming ion pairs consequently, increases in skin permeability are also due to a disruption of the stratum corneum. This conclusion was further supported by (a) increase transepidermal water loss, and (b) increased in-vivo skin permeation of the non ion-pairing methyl nicotinate, at skin sites pretreated with the fatty acids.