Division of Pharmaceutical Sciences, James L. Winkle College of Pharmacy, University of Cincinnati, Cincinnati, OH 45267, United States.
Division of Pharmaceutical Sciences, James L. Winkle College of Pharmacy, University of Cincinnati, Cincinnati, OH 45267, United States.
J Pharm Sci. 2024 Feb;113(2):407-418. doi: 10.1016/j.xphs.2023.11.008. Epub 2023 Nov 14.
In Vitro Permeation Test (IVPT) is commonly used to evaluate skin penetration of chemicals and performance of dermatological products. For a permeant with low aqueous solubility, an additive that is expected not to alter the skin barrier can be used in the receptor solution to improve permeant solubility. The objective of this study was to (a) evaluate the effects of these additives in IVPT receptor solution on skin permeability of model permeants and skin electrical resistance and (b) determine the solubility of the permeants in these receptor solutions. Bovine serum albumin (BSA), 2-hydroxypropyl-beta-cyclodextrin (HPCD), ethanol, nonionic surfactant Brij-98, and propylene glycol were the additives, and phosphate buffered saline (PBS) was the control. Steady-state skin permeability coefficients and resistances were determined. The receptor solutions examined in this study did not cause a significant increase in skin permeability or decrease in resistance (less than 40 % changes) except 25 % ethanol. The receptor solution containing 25 % ethanol induced an approximately twofold average increase in skin permeability and reduced skin electrical resistance by approximately threefold. The receptor solution of 2.5 % HPCD provided the highest levels of solubility for the model lipophilic permeants, while 0.2 % Brij-98 and 5 % ethanol showed the lowest solubility enhancement from those in PBS.
体外渗透试验(IVPT)常用于评估化学品对皮肤的渗透作用以及皮肤科产品的性能。对于水溶性低的渗透物,可以在受体溶液中添加一种预期不会改变皮肤屏障的添加剂来提高渗透物的溶解度。本研究的目的是:(a)评估这些添加剂在 IVPT 受体溶液中对模型渗透物的皮肤渗透性和皮肤电阻的影响;(b)确定这些受体溶液中渗透物的溶解度。牛血清白蛋白(BSA)、2-羟丙基-β-环糊精(HPCD)、乙醇、非离子表面活性剂 Brij-98 和丙二醇是添加剂,磷酸盐缓冲盐水(PBS)是对照。测定稳态皮肤渗透系数和电阻。本研究中检查的受体溶液并未导致皮肤渗透性显著增加或电阻显著降低(变化小于 40%),除 25%乙醇外。含 25%乙醇的受体溶液使皮肤渗透性平均增加约两倍,并使皮肤电阻降低约三倍。2.5% HPCD 的受体溶液为模型亲脂性渗透物提供了最高的溶解度水平,而 0.2% Brij-98 和 5%乙醇显示出比 PBS 中最低的溶解度增强。