Abstract
Purpose :
Ozurdex®, a dexamethasone implant injected into the eye, has been prescribed for treating macular edema associated with damage to blood vessels, non-infectious uveitis, and diabetic macular edema. The preparation contains 0.7 mg of dexamethasone with a mixture of biodegradable polymers PLGA (polylactide-co-glycolide).This study was designed to investigate the comparative ocular pharmacokinetics of dexamethasone in vitreous humour following intravitreal implantation of Ozurdex® and NDF-SI01, a new brand penetrating the market, in rabbits.
Methods :
NDF-SI01 was prepared with the same ingredients as Ozurdex®. In vitro dissolution studies for two preparations were conducted in 30 mL normal saline at 37 °C and 50 rpm using a reciprocal shaking water bath. The preparations were implanted into rabbit eyes individually, and the vitreous humor was serially taken for up to 30 days. The dexamethasone concentration was quantified using HPLC-MS/MS, and pharmacokinetic parameters were calculated.
Results :
Two implants were mostly degraded by 28 days on average. Ozurdex® and NDF-SI01 at peak 3.3 μg/mL at ~ 20.9 days and 3.1 μg/mL at ~ 19.5 days, respectively. The half-life of NDF-SI01 was 40.3 h, slightly greater than that (35.4 h) of Ozurdex®, but not statistically significant. There was no difference in AUC (684 μg h/mL for Ozurdex®; 708 μg h/mL for NDF-SI01) and clearance (1.29 mL/h for Ozurdex®; 1.27 mL/h for NDF-SI01)
Conclusions :
This work comprehensively characterized the ocular pharmacokinetics of dexamethasone implants. There was no statistical significance in all pharmacokinetic parameters for both preparations. Therefore, NDF-SI01 would be able to be interchangeable with Ozurdex®.
This abstract was presented at the 2024 ARVO Annual Meeting, held in Seattle, WA, May 5-9, 2024.