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Topical fluorouracil. Pharmacokinetics in normal rabbit eyes
Archives of Ophthalmology (Chicago, Ill. : 1960)
|July 1, 1985
Summary
Topical fluorouracil (5-FU) eye drops show promise for glaucoma surgery. This study found 5-FU penetrates rabbit eyes effectively, reaching therapeutic levels in ocular tissues for potential anti-fibrosis applications.
Area of Science:
- Ophthalmology
- Pharmacokinetics
- Drug Delivery
Background:
- Glaucoma surgery success can be limited by ocular tissue fibrosis.
- Subconjunctival fluorouracil (5-FU) injections are used to prevent failure but require invasive administration.
- Data on topical 5-FU ocular penetration are lacking.
Purpose of the Study:
- To investigate the ocular pharmacokinetics of topically administered 5-FU in a rabbit model.
- To determine if topical 5-FU achieves therapeutic concentrations in ocular tissues.
Main Methods:
- Normal rabbit eyes were treated with one or three drops of 14C-labeled 5-FU.
- Ocular tissues (conjunctiva, cornea, aqueous, lens, vitreous) and serum were collected at various time points.
- 5-FU concentrations were quantified using liquid scintillation counting.
Main Results:
- Topical 5-FU achieved significant concentrations in conjunctiva, cornea, and aqueous humor.
- Concentrations in ocular tissues were sustained for several hours post-administration.
- A 5-FU concentration of 0.2 µg/mL inhibited 50% of rabbit conjunctival fibroblast proliferation in vitro.
Conclusions:
- Topically applied 5-FU demonstrates adequate ocular penetration and achieves potentially therapeutic levels in key ocular compartments.
- Topical 5-FU represents a viable alternative to subconjunctival injections for preventing post-surgical scarring in glaucoma patients.
- Further clinical studies are warranted to confirm the efficacy and safety of topical 5-FU in glaucoma surgery.