Effects of phospholipids on the in vitro percutaneous penetration of prednisolone and analysis of mechanism by using attenuated total reflectance-Fourier transform infrared spectroscopy.
We investigated the effects of 10 phospholipids on the in vitro percutaneous penetration of prednisolone (PR) through the dorsal skin of guinea pigs. A marked enhancing effect of PR penetration was observed in the presence of phospholipids that have unsaturated acyl chains. A maximum of 68-fold enhancement was observed compared to that of control. On the contrary, phospholipids that have saturated acyl chains did not significantly increase the amount of PR passing to the receptor side. Attenuated total reflectance-Fourier transform infrared spectroscopy was used to monitor the outer several microns of stratum corneum (SC) surface. It was observed that phospholipids that have unsaturated acyl chains induced higher and broader absorbance shifts in the C-H bond stretching region while phospholipids that have saturated acyl chains induced lower and sharper absorbance shifts in the C-H bond stretching region. A significant parallel between the amount of PR penetrated and the lipid-chain fluidity of the SC was found. These results suggest that phospholipids may influence the percutaneous penetration of PR by changing the lipid-chain fluidity of the SC.
Yokomizo
Y
Y
Pharmaceutical Research Laboratories, POLA R&D Laboratories, POLA Corporation, Yokohama, Japan.
Sagitani
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H
D000818:Animals; D006168:Guinea Pigs; D008297:Male; D010743:Phospholipids / Q000494:pharmacology*; D011239:Prednisolone / Q000493:pharmacokinetics*; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption / Q000187:drug effects*; D017550:Spectroscopy, Fourier Transform Infrared
D010743:Phospholipids; D011239:Prednisolone