Sustained ocular delivery of tilisolol to rabbits after topical administration or intravitreal injection of lipophilic prodrug incorporated in liposomes.
To improve the retention time of tilisolol in the precorneal area or vitreous body, we prepared liposomes incorporating the O-palmitoyl prodrug of tilisolol. O-Palmitoyl tilisolol was completely incorporated in the liposomes. After topical administration of O-palmitoyl tilisolol liposomes to the rabbit eye, O-palmitoyl tilisolol rapidly disappeared from the tear fluid. The inclusion of 2% carmellose sodium slightly prolonged the retention of O-palmitoyl tilisolol in the tear fluid. After intravitreal injection of O-palmitoyl tilisolol liposomes, there was a relatively prolonged retention of O-palmitoyl tilisolol in the vitreous body. At 24 and 48 h after intravitreal injection of O-palmitoyl tilisolol liposomes, the tilisolol concentration in the vitreous body was significantly higher compared with the concentration after intravitreal injection of tilisolol liposomes.
Kawakami
S
S
School of Pharmaceutical Sciences, Nagasaki University, Japan.  kawakami@net.nagasaki-u.ac.jp
Yamamura
K
K
Mukai
T
T
Nishida
K
K
Nakamura
J
J
Sakaeda
T
T
Nakashima
M
M
Sasaki
H
H
D000287:Administration, Topical; D000319:Adrenergic beta-Antagonists / Q000008:administration & dosage*; D000818:Animals; D002851:Chromatography, High Pressure Liquid; D016503:Drug Delivery Systems; D007546:Isoquinolines / Q000008:administration & dosage*; D008081:Liposomes; D008297:Male; D011355:Prodrugs / Q000008:administration & dosage* / Q000378:metabolism; D011817:Rabbits; D013666:Tears / Q000378:metabolism; D014822:Vitreous Body / Q000378:metabolism
D000319:Adrenergic beta-Antagonists; D007546:Isoquinolines; D008081:Liposomes; D011355:Prodrugs; C036593:tilisolol