Effects of Tween 80 and liposomes on the corneal permeability of anti-inflammatory steroids.
The effects of Tween 80 and liposomes on the corneal permeability of dexamethasone (DM) and dexamethasone valerate (DV) were investigated in vitro. A model based on diffusion theory could successfully be applied to analyzing the process by which DM penetrates the cornea from DM preparations. The penetration rate increased according to the concentration of free DM. Although the penetration rate was increased by pretreatment with Tween 80, it was not affected by pretreatment with liposomes. The steroid that penetrated through the cornea from DV preparations had been metabolized to DM. The transfer of DM across the cornea from DV preparations tended to slow down to some extent during the penetration process. Diffusion models were not applicable to this process, in contrast to the corneal penetration of DM from DM preparations. When liposome preparations of DV were applied, the penetration rate of DM across the cornea depended the concentration of free DV in these preparations. When DV aqueous preparations containing different concentrations of Tween 80 were applied, the penetration rate increased as the concentration of the surfactant was increased, even though the concentration of free DV in the suspensions was kept constant. These results suggest that the corneal permeability of anti-inflammatory steroids is not affected by liposomes, but is accelerated by Tween 80.
Taniguchi
K
K
Research and Development Division, Rohto Pharmaceutical Co., Ltd., Osaka, Japan.
Itakura
K
K
Morisaki
K
K
Hayashi
S
S
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D003315:Cornea / Q000187:drug effects / Q000378:metabolism*; D003907:Dexamethasone / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000493:pharmacokinetics; D004058:Diffusion; D066298:In Vitro Techniques; D008081:Liposomes; D008297:Male; D008954:Models, Biological; D010539:Permeability; D011136:Polysorbates / Q000494:pharmacology*; D011817:Rabbits
D000893:Anti-Inflammatory Agents; D008081:Liposomes; D011136:Polysorbates; D003907:Dexamethasone; C030949:dexamethasone 17-valerate