Ocular Pharmacokinetics of Fluocinolone Acetonide After Retisert™ Intravitreal Implantation in Rabbits Over a 1-Year Period

Abstract

Purpose: The present study was designed to examine the pharmacokinetics of a fluocinolone acetonide (FA) intravitreal implant in pigmented rabbits. Methods: Pigmented rabbits were randomly assigned to receive either a 0.5 mg or 2.0 mg FA intravitreal implant (Retisert™). Four animals were sacrificed per time point (2 hours; 2 weeks; and 3, 6, 9, and 12 months after implantation) for FA intraocular levels determination. Results: In the vitreous, concentration of FA was relatively constant from the first time point, 2 hours, through 1 year, and dose-related, approximately seven- to eight-fold greater in the 2-mg implant. Concentrations of FA were generally higher in the vitreous (11–18 and 75–146 ng/g) and retina (42–87 and 224–489 ng/g) than in the aqueous humor (0.21–1.1 and 2.6–13.0 ng/g) for the 0.5- and 2-mg implants, respectively. Urine and plasma values were below the lower limit of quantitation (200 pg/mL) for all observations, indicating no evidence of systemic absorption. Conclusions: In this rabbit study, the Retisert™ provides relatively constant levels of FA in the posterior pole, which is consistent with previous reports of its clinical utility.