Sloan Kenneth B, Devarajan-Ketha Hemamalini, Synovec Jennifer, Majumdar Susruta
Department of Medicinal Chemistry, University of Florida, Gainesville, FL, USA.
J Cosmet Sci. 2013 May-Jun;64(3):181-92.
It would be useful to develop a surrogate for animal skin, which could be use to predict flux through human skin. The fluxes (and physicochemical properties) of sunscreens and other compounds from propylene glycol (PG):water (AQ), 30:70, through human skin have previously been reported. We measured the fluxes of several of those sunscreens and other compounds from PG:AQ, 30:70, through silicone membrane and fit both sets of data to the Roberts-Sloan (RS) equation to determine any similarities. For both sets of data, the fluxes were directly dependent on their solubilities in a lipid solvent [octanol (OCT), in this case] and in a polar solvent (PG:AQ, 30:70, or AQ in this case) and inversely on their molecular weights. The fit of the experimental (EXP) fluxes through human skin in vivo to RS was excellent: r² = 0.92 if the vehicle (VEH) PG:AQ, 30:70 was the polar solvent (RS¹) or r² = 0.97 if water was the polar solvent (RS²). The fit of the EXP fluxes through silicone membrane to RS was good: r² = 0.80 if the VEH PG:AQ, 30:70, was the polar solvent (RS¹) or r² = 0.81 if water was the polar solvent (RS²). The correlations between their EXP fluxes through human skin in vivo and their EXP fluxes through silicone membrane were good (r² = 0.85). In addition, the correlation between EXP fluxes from PG:AQ, 30:70, through human skin in vivo and their fluxes calculated from the coefficients of the fit of solubilities, molecular weights and fluxes from water through silicone membranes from a previous n = 22 database to RS was even better (r² = 0.94). These results suggest that flux through human skin can be calculated from flux through a silicone membrane.
开发一种动物皮肤替代品将很有用，它可用于预测经人体皮肤的通量。先前已报道了防晒剂和其他化合物从丙二醇（PG）:水（AQ）（30:70）透过人体皮肤的通量（以及物理化学性质）。我们测量了其中几种防晒剂和其他化合物从PG:AQ（30:70）透过硅酮膜的通量，并将两组数据拟合到罗伯茨 - 斯隆（RS）方程以确定任何相似性。对于两组数据，通量直接取决于它们在脂质溶剂（在这种情况下为辛醇（OCT））和极性溶剂（在这种情况下为PG:AQ，30:70，或AQ）中的溶解度，并且与它们的分子量成反比。体内经人体皮肤的实验（EXP）通量与RS的拟合非常好：如果载体（VEH）PG:AQ，30:70是极性溶剂（RS¹），则r² = 0.92；如果水是极性溶剂（RS²），则r² = 0.97。经硅酮膜的EXP通量与RS的拟合良好：如果VEH PG:AQ，30:70是极性溶剂（RS¹），则r² = 0.80；如果水是极性溶剂（RS²），则r² = 0.81。它们在体内经人体皮肤的EXP通量与经硅酮膜的EXP通量之间的相关性良好（r² = 0.85）。此外，从PG:AQ，30:70经体内人体皮肤的EXP通量与根据先前n = 22的数据库中从水透过硅酮膜的溶解度、分子量和通量的拟合系数计算出的通量之间的相关性甚至更好（r² = 0.94）。这些结果表明，可以根据经硅酮膜的通量来计算经人体皮肤的通量。
