title: Sustained ocular delivery of tilisolol to rabbits after topical administration or intravitreal injection of lipophilic prodrug incorporated in liposomes.
abstract: 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.
authors.affiliation: School of Pharmaceutical Sciences, Nagasaki University, Japan.  kawakami@net.nagasaki-u.ac.jp
authors.forename: S
authors.initials: S
authors.lastname: Kawakami
authors.forename: K
authors.initials: K
authors.lastname: Yamamura
authors.forename: T
authors.initials: T
authors.lastname: Mukai
authors.forename: K
authors.initials: K
authors.lastname: Nishida
authors.forename: J
authors.initials: J
authors.lastname: Nakamura
authors.forename: T
authors.initials: T
authors.lastname: Sakaeda
authors.forename: M
authors.initials: M
authors.lastname: Nakashima
authors.forename: H
authors.initials: H
authors.lastname: Sasaki
mesh_terms: 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
chemical_list: D000319:Adrenergic beta-Antagonists; D007546:Isoquinolines; D008081:Liposomes; D011355:Prodrugs; C036593:tilisolol