PURPOSE: Compound permeation through stratum corneum-stripped skin is generally greater than that through full-thickness skin. In addition, epidermis-to-dermis permeation profile should be the same as dermis-to-epidermis permeation profile. However, stripped skin permeability of some compounds was lower than full-thickness skin permeability and different permeabilities were found for some compounds between the two directions of skin permeation. The reasons for these findings were investigated in this study. METHODS: Full-thickness or stripped hairless rat skin was set in a Franz-type diffusion cell, and a solution of compound was applied on the epidermis or dermis side to determine the in vitro skin permeability. RESULTS: Although the stripped skin permeability of pentyl paraben (PeP) with extremely high logK(o/w) was lower than full-thickness skin permeabilities, the addition of 3% ethanol resulted in the expected permeation order. Epidermis-to-dermis permeation of PeP through full-thickness skin was higher than dermis-to-epidermis permeation. Epidermis-to-dermis permeations of fluorescein isothiocyanate dextran (FD-4) and isosorbide 5-mononitrate with negative logK(o/w) were also higher than those in the opposite direction. CONCLUSIONS: Morphological observation of skin after FD-4 permeation suggested that a conically shaped trans-follicular permeation pathway model could be advocated to explain the difference between the epidermis-to-dermis permeation and that in the opposite direction.
PURPOSE: Compound permeation through stratum corneum-stripped skin is generally greater than that through full-thickness skin. In addition, epidermis-to-dermis permeation profile should be the same as dermis-to-epidermis permeation profile. However, stripped skin permeability of some compounds was lower than full-thickness skin permeability and different permeabilities were found for some compounds between the two directions of skin permeation. The reasons for these findings were investigated in this study. METHODS: Full-thickness or stripped hairless rat skin was set in a Franz-type diffusion cell, and a solution of compound was applied on the epidermis or dermis side to determine the in vitro skin permeability. RESULTS: Although the stripped skin permeability of pentyl paraben (PeP) with extremely high logK(o/w) was lower than full-thickness skin permeabilities, the addition of 3% ethanol resulted in the expected permeation order. Epidermis-to-dermis permeation of PeP through full-thickness skin was higher than dermis-to-epidermis permeation. Epidermis-to-dermis permeations of fluorescein isothiocyanate dextran (FD-4) and isosorbide 5-mononitrate with negative logK(o/w) were also higher than those in the opposite direction. CONCLUSIONS: Morphological observation of skin after FD-4 permeation suggested that a conically shaped trans-follicular permeation pathway model could be advocated to explain the difference between the epidermis-to-dermis permeation and that in the opposite direction.