0000000001064586
AUTHOR
A. Copoví
Enhancing effect of alpha-hydroxyacids on "in vitro" permeation across the human skin of compounds with different lipophilicity.
The percutaneous penetration-enhancing effects of glycolic acid, lactic acid and sodium lauryl sulphate through the human epidermis was investigated using 5-fluorouracil as a hydrophilic model permeant and three compounds belonging to the phenylalcohols: 2-phenyl-ethanol, 4-phenyl-butanol and 5-phenyl-pentanol. The lipophilicity values of the compounds ranged from log Poct -0.95 to 2.89. The effect of the enhancer concentration was also studied. Skin pretreatment with aqueous solutions of the three enhancers did not increase the permeability coefficient of the most lipophilic compound (log Poct = 2.89). For the other compounds assayed, the increase in the permeability coefficients depended …
A modelistic approach showing the importance of the stagnant aqueous layers in in vitro diffusion studies, and in vitro-in vivo correlations
Abstract The present study deals with the role of the aqueous diffusion layers on the in vitro penetration of xenobiotics across artificial lipoidal membranes, and their ability to reproduce biophysical absorption models when in vivo results are to be simulated from the in vitro tests. The aqueous boundary layers which are invariably formed on artificial lipoidal membranes can be optionally preserved or disrupted, according to the type of absorption site which should be simulated, a condition which could reasonably lead to a better correspondence between in vitro and in vivo results; in practice, disruption of water layers can be easily achieved by a synthetic surfactant solution at its cri…