Efficacy of a liposome preparation of anti-inflammatory steroid as an ocular drug-delivery system.
The efficacy of a liposome preparation on ocular steroid availability was investigated by both tracer studies and investigation of in vivo steroid uptake by the cornea. Dexamethasone and its ester derivatives were used as model drugs and aqueous suspensions of each served as control preparations. The liposome preparation containing dexamethasone valerate provided the highest ocular drug levels among the examined preparations. In the case of dexamethasone or dexamethasone palmitate, the liposomal form provided a lower drug level in comparison with the suspension. High esterase activity for dexamethasone valerate was observed in the corneal homogenate supernatant, and most of the steroid taken up after instillation of dexamethasone valerate was metabolized to free alcohol. The corneal dexamethasone level was almost proportional to the concentration of free dexamethasone valerate in the liposome preparation. Only the addition of stearylamine (SA) to the liposomal membrane had an added extra effect on the corneal absorption of dexamethasone valerate.
Taniguchi
K
K
Research and Development Division, Rohto Pharmaceutical Co., Ltd., Osaka, Japan.
Itakura
K
K
Yamazawa
N
N
Morisaki
K
K
Hayashi
S
S
Yamada
Y
Y
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000627:therapeutic use*; D003315:Cornea / Q000201:enzymology; D003907:Dexamethasone / Q000627:therapeutic use; D005128:Eye Diseases / Q000188:drug therapy*; D008081:Liposomes / Q000008:administration & dosage*; D011817:Rabbits
D000893:Anti-Inflammatory Agents; D008081:Liposomes; D003907:Dexamethasone