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. 2021 May 18:15:2055-2061.
doi: 10.2147/OPTH.S307194. eCollection 2021.

Plasma Pharmacokinetic Parameters of Dexamethasone Following Administration of a Dexamethasone Intracanalicular Insert in Healthy Adults

Charles Blizzard  1 , Eugene B McLaurin  2 , Arthur Driscoll  1 , Fabiana Q Silva  1 , Srilatha Vantipalli  1 , Jamie Lynne Metzinger  1 , Michael H Goldstein  1
Affiliations

Plasma Pharmacokinetic Parameters of Dexamethasone Following Administration of a Dexamethasone Intracanalicular Insert in Healthy Adults

Charles Blizzard et al. Clin Ophthalmol. .

Abstract

Purpose: Intracanalicular dexamethasone insert is a resorbable sustained-release polyethylene glycol-based hydrogel insert delivering a 0.4 mg tapered dose of dexamethasone for up to 30 days to the ocular surface. It is FDA-approved for treating inflammation and pain after ocular surgery. It has also been studied for ocular surface diseases such as allergic conjunctivitis. This study assessed the plasma pharmacokinetic (PK) parameters of dexamethasone following intracanalicular insertion.

Patients and methods: Study subjects (N=16) were healthy adults. A dexamethasone insert was unilaterally placed into the canaliculus, and blood samples were obtained for analysis 1 hour prior to insertion and 1, 2, 4, 8, 16, 24 hours and 4, 8, 15, 22 and 29 days after insertion. Safety analyses included slit lamp and dilated fundus examinations, best corrected visual acuity, intraocular pressure (IOP) and adverse events (AEs).

Results: Plasma results were below the lower limit of quantitation (LLOQ) at all time points in five subjects (31.3%). Among subjects with quantifiable plasma concentrations, Cmax was <1 ng/mL (range, 0.05 to 0.81 ng/mL), AUC0-last ranged from 0.13 to 7.18 h∙ng/mL, and Tmax ranged from 4.0 to 163.0 hours. Mean (SD) IOP increased from 16.3 (1.4) mmHg at baseline to 19.3 (3.2) at Day 22 but returned to baseline after treatment. No changes occurred in dilated fundus, punctum, or visual acuity examinations.

Conclusion: The dexamethasone 0.4 mg insert results in minimal systemic exposure following intracanalicular administration.

Keywords: intracanalicular dexamethasone; plasma pharmacokinetics; safety assessments; sustained-release insert.

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Conflict of interest statement

Michael H Goldstein, Srilatha Vantipalli, Jamie Lynne Hart, Fabiana Q Silva, Charles Blizzard, and Arthur Driscoll are employees of and owned stocks for Ocular Therapeutix who was the sponsor for the study and who commercializes DEXTENZA. Mr Charles Blizzard has a patent issued: US20160331738A1 - Drug Delivery Through Hydrogels. Eugene B McLaurin is affiliated with Total Eye Care and is an investigator in a clinical trial sponsored by Ocular Therapeutix. The authors report no other conflicts of interest in this work.

Figures

Figure 1
Figure 1
The dexamethasone insert is placed in the punctum and into the canaliculus.
See this image and copyright information in PMC

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