Tanojo H, Boelsma E, Junginger H E, Ponec M, Boddé H E
Division Pharmaceutical Technology, Leiden/Amsterdam Center for Drug Research, Leiden University, The Netherlands.
Skin Pharmacol Appl Skin Physiol. 1998 Mar-Apr;11(2):87-97. doi: 10.1159/000029813.
The in vivo effects of fatty acids on skin barrier function were assessed by measuring: (i) transepidermal water loss (TEWL), (ii) diffusion lag times for hexyl nicotinate (HN), and (iii) irritant skin response using laser Doppler velocimetry (LDV) in combination with visual scoring. Two classes of fatty acids have been investigated: straight-chain saturated fatty acids (SFA), having 6-12 carbon atoms, and unsaturated fatty acids (UFA): oleic, linoleic, alpha-linolenic and arachidonic acids. It has been reported that these acids can enhance the permeation of various compounds across the skin. After topical and occlusive application as a solution in propylene glycol (PG) for 3 h on the volar arm of human subjects, SFA only caused a slight irritation and increase in TEWL. The diffusion lag times of HN were reduced by the application SFA to the same extent as and not more than by the application of the pure solvent PG. In contrast, the application of UFA caused a significant increase in TEWL and LDV (irritation) responses. The TEWL values after oleic acid application were higher than those observed for the other three acids, while the irritation potential of arachidonic acid was the highest among UFA. As with SFA, sites treated with UFA did not show significantly different lag times of HN diffusion from PC-treated sites. The data suggest that the degree of irritation and the degree of barrier modulation for fatty acids are not necessarily correlated.
（i）经表皮水分流失（TEWL）；（ii）烟酸己酯（HN）的扩散滞后时间；（iii）使用激光多普勒测速仪（LDV）结合视觉评分法评估刺激性皮肤反应。研究了两类脂肪酸：具有6至12个碳原子的直链饱和脂肪酸（SFA）和不饱和脂肪酸（UFA）：油酸、亚油酸、α-亚麻酸和花生四烯酸。据报道，这些酸可增强各种化合物透过皮肤的渗透能力。在人体受试者的掌臂上以丙二醇（PG）溶液局部封闭涂抹3小时后，SFA仅引起轻微刺激并使TEWL增加。HN的扩散滞后时间因涂抹SFA而缩短，其程度与涂抹纯溶剂PG相同且不超过后者。相比之下，涂抹UFA会导致TEWL和LDV（刺激）反应显著增加。涂抹油酸后的TEWL值高于其他三种酸，而花生四烯酸在UFA中的刺激潜力最高。与SFA一样，用UFA处理的部位与用PG处理的部位相比，HN扩散的滞后时间没有显著差异。数据表明，脂肪酸的刺激程度和屏障调节程度不一定相关。
