Prediction of Skin Permeability of Drugs: Comparison of Human and Hairless Rat Skin

Abstract

Relationships between skin permeability and physicochemical properties of drugs were examined to establish a predictive method for the steady-state permeation rate of drugs through human skin. Human skin permeation properties fell into two categories: one in which the permeability coefficient is correlated to the partition coefficient, revealed with lipophilic drugs; and the other in which the permeability coefficients are almost constant, shown with hydrophilic drugs. The stratum corneum, the main barrier in skin, could be considered as a membrane with two parallel permeation pathways: lipid and pore pathways, and an equation for predicting the steady-state permeation rate of drugs was derived. The skin permeabilities of drugs for man were compared with those for hairless rat. The species difference in skin permeability found was suggested to be due to the difference in skin permeation pathways, since lipid content and water uptake of the stratum corneum varied between human and hairless rat skin.

Comparative Permeation Studies between Scale Region of Shed Snake Skin and Human Skin In vitro

“…Its permeation was, thus, rather low and slow and its lag time was found to be approximately 4 h which is similar to that reported by Morimoto et al [22] . Additionally, when comparison to salicylic acid, diclofenac sodium permeated much slower, similar to the results of Gabboun et al [23] .…”

Usefulness of Rat Skin as a Substitute for Human Skin in the in Vitro Skin Permeation Study

“…In this study, we used human abdominal skins from 6 humans and selected three model drugs with different partition coefficients [11,16,18,26,32]. The log K ow values of NR, ISDN, and FP are -1.02 (low), 1.34 (intermediate), and 3.86 (high), respectively.…”

“…NR, ISDN, and FP are used as hydrophilic, lipophilic, and highly lipophilic drugs, respectively. The stratum corneum is a membrane with a lipid pathway and a pore pathway, which serve as the main routes for lipophilic and hydrophilic drugs, respectively [16,18].…”

“…The three model drugs were selected because of their different log K ow (logarithm of the octanol/water partition coefficient at 37ºC; Table 1). NR, ISDN, and FP were used as hydrophilic, lipophilic, and highly lipophilic drugs, respectively [11,16,18,26,33].…”

A Novel Chemical Enhancer Approach for Transdermal Drug Delivery with C₁₇-Monoglycerol Ester Liquid Crystal-forming Lipid

“…Correlation of skin permeation of chemicals to human skin is very important, previous studies showed a good relationships of skin permeation of chemicals between human and hairless rat skin 41,42 . Significant improvement in the skin permeation of different drugs was observed after application of MGE and GMO formulations Fig.…”