Abstract | PURPOSE: In the topical delivery of drugs to the lens, drug retention on the eye surface is considered to be important because increased retention on the ocular surface should lead to increased ocular absorption of a drug through the cornea into the aqueous humor and subsequently the lens. The aim of this study was to investigate whether increasing the viscosity of a topical aldose reductase inhibitor suspension increases the lenticular bioavailability of the inhibitor and whether such a formulation can arrest sugar cataract formation. METHODS: RESULTS: Lenticular levels of 2-MS was highest in rats administered suspensions containing 0.25% carbopol + 0.25% HPMC as vehicles followed by 0.5% gellan gum, 0.5% HPMC, 0.25% carbopol, and 0.5% xanthan gum. All untreated rats fed a 50% galactose diet developed hypermature cataracts within 15 days; however, none of the topical treated rats demonstrated cortical vacuole formation after 21 days of galactose feeding. CONCLUSIONS: In the suspensions examined, no direct relationship between the lenticular drug levels of 2-MS and either viscosity or pH of the vehicles were observed. The observed arrest of sugar cataract formation indicated that therapeutically adequate lenticular levels of 2-MS were provided by all topical suspensions.
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Authors | Peter F Kador, James Randazzo, Thomas Babb, Kavitha Koushik, Yoshihiro Takamura, Wenjun Zhu, Karen Blessing, Uday B Kompella |
Journal | Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics
(J Ocul Pharmacol Ther)
Vol. 23
Issue 2
Pg. 116-23
(Apr 2007)
ISSN: 1080-7683 [Print] United States |
PMID | 17444799
(Publication Type: Journal Article)
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Chemical References |
- Drug Carriers
- Enzyme Inhibitors
- Imidazolidines
- Ophthalmic Solutions
- Pharmaceutical Vehicles
- M 79175
- Aldehyde Reductase
- Galactose
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Topics |
- Administration, Topical
- Aldehyde Reductase
(antagonists & inhibitors)
- Animals
- Aqueous Humor
- Biological Availability
- Biological Transport
- Cataract
(chemically induced, drug therapy)
- Cornea
- Drug Carriers
- Enzyme Inhibitors
(administration & dosage, pharmacokinetics, pharmacology)
- Galactose
- Hydrogen-Ion Concentration
- Imidazolidines
(administration & dosage, pharmacokinetics, pharmacology)
- Lens, Crystalline
(drug effects, physiopathology)
- Male
- Mydriasis
- Ophthalmic Solutions
(administration & dosage, pharmacokinetics, pharmacology)
- Pharmaceutical Vehicles
- Rats
- Rats, Sprague-Dawley
- Vacuoles
- Viscosity
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