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 rab...

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Bibliographic Details
Published in:Journal of pharmacy and pharmacology 2001-08, Vol.53 (8), p.1157-1161
Main Authors: Kawakami, Shigeru, Yamamura, Kenzo, Mukai, Takahiro, Nishida, Koyo, Nakamura, Junzo, Sakaeda, Toshiyuki, Nakashima, Mikiro, Sasaki, Hitoshi
Format: Article
Language:English
Subjects:
Administration, Topical
Adrenergic beta-Antagonists - administration & dosage
Animals
Chromatography, High Pressure Liquid
Drug Delivery Systems
Isoquinolines - administration & dosage
Liposomes
Male
Prodrugs - administration & dosage
Prodrugs - metabolism
Rabbits
Tears - metabolism
Vitreous Body - metabolism
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Summary: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.
ISSN:0022-3573
2042-7158
DOI:10.1211/0022357011776423