Bashir S J, Dreher F, Chew A L, Zhai H, Levin C, Stern R, Maibach H I
Department of Dermatology, University of California, 90 Medical Center Way, Surge Building #110, P.O. Box 0989, San Francisco, CA 94143-0989, USA.
Int J Pharm. 2005 Mar 23;292(1-2):187-94. doi: 10.1016/j.ijpharm.2004.11.032. Epub 2005 Jan 26.
Keratolytic efficacy of topical preparations containing salicylic acid was studied in humans utilizing adhesive tape stripping and quantifying SC removal by protein analysis. In combination with tape stripping, squamometry was used to evaluate the influence of salicylic acid on skin surface scaliness and desquamation. Furthermore, skin barrier perturbation and skin irritancy was recorded and related to the dermatopharmacological effect of the preparations. In contrast to squamometry, tape stripping combined with protein analysis was sensitive in detecting keratolytic effect of salicylic acid within hours of application. Importantly, whereas the pH of the preparations only minimally influenced efficacy, local dermatotoxicity was significantly increased at acidic pH. This indicates that the quest to increase the amount of free, non-dissociated SA is, in fact, counterproductive as the more acidic preparations resulted in skin irritation and barrier disruption.
利用胶带剥离法并通过蛋白质分析对去除的角质层进行定量，研究了含水杨酸的外用制剂在人体中的角质溶解功效。结合胶带剥离法，使用鳞屑测量法评估水杨酸对皮肤表面鳞屑和脱屑的影响。此外，记录皮肤屏障扰动和皮肤刺激性，并将其与制剂的皮肤药理学效应相关联。与鳞屑测量法不同，胶带剥离法结合蛋白质分析在应用数小时内就能灵敏地检测出水杨酸的角质溶解作用。重要的是，虽然制剂的pH值对功效影响极小，但在酸性pH值下局部皮肤毒性会显著增加。这表明，事实上，增加游离、未解离水杨酸量的做法适得其反，因为酸性更强的制剂会导致皮肤刺激和屏障破坏。
