Kinetics of topically administered prednisolone acetate. Optimal concentration for treatment of inflammatory...

Two types of quantitative measurements were made in rabbit corneas. First, the level that varying concentrations of topically administered prednisolone acetate attained in the cornea and aqueous humor was determined. Then, the ability of varying concentrations of this corticosteroid to suppress corneal inflammation was ascertained. The maximum dose-response curve for anti-inflammatory effect in the cornea was achieved by the 1.0% concentration, the highest concentration commercially available. Higher concentrations permitted greater quantities of the drug to gain access to the cornea and aqueous humor but produced no measurable increment in anti-inflammatory effect. These experimental observations suggest that concentrations of prednisolone acetate higher than 1.0% have an increased potential for toxicity without offering additional therapeutic benefit.