Objective: To observe the penetration of 0.5% fluconazole (FCZ) into the corneas and aqueous humors of New Zealand white rabbits following its topical application.
Methods: The rabbit corneas and aqueous humors were obtained and quantified at different times after topically applying 0.5% FCZ to the rabbit eyes. The drug levels were assayed by high performance liquid chromatography (HPLC). The pharmacokinetic parameters were calculated with nonlinear least square method by the computer.
Results: FCZ can rapidly penetrate into rabbit corneas. Peak corneal levels occurred essentially immediately at 2 min in the corneas (15.20 +/- 1.95) microgram/g and at 15 min after application in the aqueous (2.39 +/- 0.92 mg/L). The permeability of the corneal epithelial barrier (Kep) was 1.06 x 10(-5). The half-life (t(l/2)) of the cornea was 63.96 min, and that of the aqueous humor was 42.14 min.
Conclusion: Topical fluconazole can be used as a topical antifungal agent to treat keratitis and needs further evaluation for treating fungal endophthalmitis.