Sustained ocular delivery of tilisolol to rabbits after topical administration or intravitreal injection of lipophilic prodrug incorporated in liposomes

• Published in: Journal of pharmacy and pharmacology Vol. 53; no. 8; p. 1157
• Main Authors: Kawakami, S, Yamamura, K, Mukai, T, Nishida, K, Nakamura, J, Sakaeda, T, Nakashima, M, Sasaki, H
• Format: Journal Article
• Language: English
• Published: England 01.08.2001
• 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
• ISSN: 0022-3573
• DOI: 10.1211/0022357011776423

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.