Topical pharmacokinetics of dexamethasone suspensions in the rabbit eye: Bioavailability comparison

[Display omitted] Topical corticosteroids are used to treat inflammation of the anterior segment. Due to their low water-solubility, they are often formulated as suspensions, but ocular bioavailability of the suspensions is not known. Herein, ocular pharmacokinetics of dexamethasone in albino rabbit...

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Bibliographic Details
Published in:International journal of pharmaceutics 2022-03, Vol.615, p.121515-121515, Article 121515
Main Authors: Naageshwaran, Vatsala, Ranta, Veli-Pekka, Toropainen, Elisa, Tuomainen, Marjo, Gum, Glenwood, Xie, Enli, Bhoopathy, Siddhartha, Urtti, Arto, del Amo, Eva M.
Format: Article
Language:English
Subjects:
Administration, Topical
Animals
Aqueous Humor
Biological Availability
Clearance
Cornea
Dexamethasone
Eye
Intracameral
Ocular bioavailability
Ocular suspension
Ophthalmic Solutions
Pharmacokinetics
Rabbits
Suspensions
Topical
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Summary:[Display omitted] Topical corticosteroids are used to treat inflammation of the anterior segment. Due to their low water-solubility, they are often formulated as suspensions, but ocular bioavailability of the suspensions is not known. Herein, ocular pharmacokinetics of dexamethasone in albino rabbits was investigated following intracameral administration of dexamethasone solution and topical administration of three commercial suspensions: Maxidex®, TobraDex®, and TobraDexST®. Dexamethasone concentrations in tear fluid, cornea, aqueous humor, conjunctiva and iris-ciliary body were determined. Non-compartmental analysis was performed to estimate the pharmacokinetic parameters of dexamethasone. Following intracameral administration, the clearance and the apparent volume of distribution were estimated to be 13.6 µL/min and 990 µL, respectively. After topical administration, the absolute aqueous humor bioavailability for dexamethasone (
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2022.121515