EFFECTS OF PHOSPHOLIPIDS ON THE IN-VITRO PERCUTANEOUS PENETRATION OF PREDNISOLONE AND ANALYSIS OF MECHANISM BY USING ATTENUATED TOTAL REFLECTANCE FOURIER-TRANSFORM INFRARED-SPECTROSCOPY
Y. Yokomizo et H. Sagitani, EFFECTS OF PHOSPHOLIPIDS ON THE IN-VITRO PERCUTANEOUS PENETRATION OF PREDNISOLONE AND ANALYSIS OF MECHANISM BY USING ATTENUATED TOTAL REFLECTANCE FOURIER-TRANSFORM INFRARED-SPECTROSCOPY, Journal of pharmaceutical sciences, 85(11), 1996, pp. 1220-1226
We investigated the effects of 10 phospholipids on the in vitro percut
aneous penetration of prednisolone (PR) through the dorsal skin of gui
nea pigs. A marked enhancing effect of PR penetration was observed in
the presence of phospholipids that have unsaturated acyl chains. A max
imum 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 s
tretching region while phospholipids that have saturated acyl chains i
nduced 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 t
hat phospholipids may influence the percutaneous penetration of PR by
changing the lipid-chain fluidity of the SC.