+ Site Statistics
+ Search Articles
+ PDF Full Text Service
How our service works
Request PDF Full Text
+ Follow Us
Follow on Facebook
Follow on Twitter
Follow on LinkedIn
+ Subscribe to Site Feeds
Most Shared
PDF Full Text
+ Translate
+ Recently Requested

Ocular absorption behavior of palmitoyl tilisolol, an amphiphilic prodrug of tilisolol, for ocular drug delivery

Ocular absorption behavior of palmitoyl tilisolol, an amphiphilic prodrug of tilisolol, for ocular drug delivery

Journal of Pharmaceutical Sciences 90(12): 2113-2120

The objective of this study was to examine the ocular absorption behavior of an amphiphilic prodrug after instillation onto the cornea of rabbits. A micellar solution of O-palmitoyl tilisolol (PalTL), an amphiphilic prodrug, was prepared. After instillation of tilisolol (TL) and PalTL, the drug concentrations in the tear fluid, cornea, aqueous humor, iris-ciliary body, vitreous body, and blood were measured. In addition, in situ ocular absorption behavior was also evaluated. After instillation of TL, the concentration of TL in the tear fluid quickly decreased. After instillation of PalTL, prolonged retention and high concentrations of PalTL in tear fluid and the cornea were observed. In addition, more prolonged retention of the TL concentration after instillation of PalTL than after instillation of TL was observed in the cornea, aqueous humor, and iris-ciliary body. In situ experiments demonstrated that PalTL was mainly absorbed by the corneal route and the improvement effects of PalTL under in vivo conditions was due to an enhanced transit time of PalTL in ocular tissues. PalTL, an amphiphilic prodrug, exhibited increased retention in the precorneal area compared with the parent drug, TL, resulted in improved ocular absorption of the parent drug.

Please choose payment method:

(PDF emailed within 0-6 h: $19.90)

Accession: 011083207

Download citation: RISBibTeXText

PMID: 11745770

DOI: 10.1002/jps.1162

Related references

Biodistribution and pharmacokinetics of O-palmitoyl tilisolol, a lipophilic prodrug of tilisolol, after intravenous administration in rats. Biological & Pharmaceutical Bulletin 25(8): 1072-1076, 2002

Ocular delivery of the β-blocker, tilisolol, through the prodrug approach. International Journal of Pharmaceutics 93(1-3): 49-60, 1993

Ocular delivery of the beta-blocker, tilisolol, through the prodrug approach. International Journal of Pharmaceutics 93(1-3): 49-60, 1993

Sustained ocular delivery of tilisolol to rabbits after topical administration or intravitreal injection of lipophilic prodrug incorporated in liposomes. Journal of Pharmacy and Pharmacology 53(8): 1157-1161, 2001

In situ ocular absorption of tilisolol through ocular membranes in albino rabbits. Journal of Pharmaceutical Sciences 85(9): 940-943, 1996

Controlled release and ocular absorption of tilisolol utilizing ophthalmic insert-incorporated lipophilic prodrugs. Journal of Controlled Release 76(3): 255-263, 19 October, 2001

Characterization of ocular pharmacokinetics of tilisolol after instillation into anesthetized rabbits. Biological & Pharmaceutical Bulletin 22(11): 1253-1255, 1999

Ocular permeability of FITC-dextran with absorption promoter for ocular delivery of peptide drug. Journal of Drug Targeting 3(2): 129-135, 1995

Controlled drug delivery devices for experimental ocular studies with timolol 2. ocular and systemic absorption in rabbits. International Journal of Pharmaceutics 61(3): 241-250, 1990

A timolol prodrug for improved ocular delivery: Synthesis, conformational study and hydrolysis of palmitoyl timolol malonate. International Journal of Pharmaceutics (Amsterdam) 128(1-2): 179-188, 1996

Prodrug Strategies in Ocular Drug Delivery. Medicinal Chemistry 8(4): 753-768, 2012

Prodrug strategies in ocular drug delivery. Medicinal Chemistry ) 8(4): 753-768, 2012

Novel drug delivery systems for ocular therapy: With special reference to liposomal ocular delivery. European Journal of Ophthalmology 29(1): 113-126, 2019

Ocular drug metabolism of the bioactivating antioxidant N-acetylcarnosine for vision in ophthalmic prodrug and codrug design and delivery. Drug Development and Industrial Pharmacy 34(10): 1071-1089, 2008

Ocular Drug Distribution and Safety of a Noninvasive Ocular Drug Delivery System of Dexamethasone Sodium Phosphate in Rabbit. Journal of Ocular Pharmacology and Therapeutics 34(4): 325-334, 2018