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Pharmacokinetics of Intraocular Drug Delivery by Periocular Injections Using Ocular Fluorophotometry

From the Emory University Eye Center, Atlanta, Georgia.

PURPOSE. To evaluate the pharmacokinetics of the periocular injections: posterior subtenon (PST), retrobulbar (RB), and subconjunctival (SC) injection.

METHODS. Two sodium fluorescein (NaF) concentrations, 2.5 mg in 0.1 mL (NaF1) and 2.5 mg in 0.5 mL (NaF2) were injected into live rabbits by the PST (NaF1 n = 4, NaF2 n = 3), RB (NaF1 n = 10), SC (NaF1 n = 6), and intravenous (IV, NaF1 n = 6) routes and into euthanatized rabbits by the RB (NaF1 n = 8) route. NaF concentrations in the choroid/retina, vitreous, and anterior segment were measured by ocular fluorophotometry. The NaF level in the contralateral choroid/retina was used as a measure of the systemic drug levels.

RESULTS. The maximum NaF concentrations (nanograms per milliliter) in the choroid/retina after PST, RB, SC, and IV were 757 ± 549 at 2 hours, 906 ± 1014 at 1 hour, 320 ± 462 at 2 hours, and 865 ± 363 at 5 to 10 minutes, respectively. The PST had the highest and most prolonged vitreous NaF1 concentration (maximum: 270 ± 226 ng/mL at 3.5 hours). The contralateral peak choroid/retina NaF levels after the RB, SC, and IV injections were 7, 4, and 21 times greater than after the PST injection. The SC injection had the highest anterior segment NaF concentration (5364 ± 2840 ng/mL at 2 hours). PST with NaF2 resulted in intraocular NaF levels higher than with NaF1.

CONCLUSIONS. NaF reaches the choroid/retina by transscleral diffusion from the periocular depot. The orbital and conjunctival vasculature and lymphatics have a larger role in NaF clearance than does the choroid. NaF diffuses into the vitreous from the choroid and the anterior segment; the periocular depot location determines the predominant diffusion pathway. The duration of high NaF levels in the choroid/retina or the anterior segment determines vitreous NaF levels. PST is the best periocular route for vitreous NaF delivery with minimal systemic levels. Increasing the volume of NaF PST depot enhances transscleral drug delivery.

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