Expression, activity and pharmacokinetic impact of ocular transporters

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http://hdl.handle.net/10138/307629

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Vellonen , K-S , Hellinen , L , Mannermaa , E , Ruponen , M , Urtti , A & Kidron , H 2018 , ' Expression, activity and pharmacokinetic impact of ocular transporters ' , Advanced Drug Delivery Reviews , vol. 126 , pp. 3-22 . https://doi.org/10.1016/j.addr.2017.12.009

Title: Expression, activity and pharmacokinetic impact of ocular transporters
Author: Vellonen, Kati-Sisko; Hellinen, Laura; Mannermaa, Eliisa; Ruponen, Marika; Urtti, Arto; Kidron, Heidi
Contributor: University of Helsinki, Faculty of Pharmacy
University of Helsinki, Drug Research Program
Date: 2018-02-15
Language: eng
Number of pages: 20
Belongs to series: Advanced Drug Delivery Reviews
ISSN: 0169-409X
URI: http://hdl.handle.net/10138/307629
Abstract: The eye is protected by several tissues that limit the permeability and entry of potentially harmful substances, but also hamper the delivery of drugs in the treatment of ocular diseases. Active transport across the ocular barriers may affect drug distribution, but the impact of drug transporters on ocular drug delivery is not well known. We have collected and critically reviewed the literature for ocular expression and activity of known drug transporters. The review concentrates on drug transporters that have been functionally characterized in ocular tissues or primary cells and on transporters for which there is available expression data at the protein level. Species differences are highlighted, since these may explain observed inconsistencies in the influence of specific transporters on drug disposition. There is variable evidence about the pharmacokinetic role of transporters in ocular tissues. The strongest evidence for the role of active transport is available for the blood-retinal barrier. We explored the role of active transport in the cornea and blood retinal barrier with pharmacokinetic simulations. The simulations show that the active transport is important only in the case of specific parameter combinations. (C) 2017 Elsevier B.V. All rights reserved.
Subject: Active transport
Blood-retinal barrier
Blood-aqueous barrier
Conjunctiva
Cornea
Neural retina
Pharmacogenetics
BLOOD-RETINAL BARRIER
CORNEAL EPITHELIAL-CELLS
AMINO-ACID TRANSPORTER
INTRAOCULAR-PRESSURE RESPONSE
TARGETED ABSOLUTE PROTEOMICS
ORGANIC CATION TRANSPORTERS
CARRIER-MEDIATED TRANSPORT
AQUEOUS HUMOR BARRIER
OPEN-ANGLE GLAUCOMA
P-GLYCOPROTEIN
317 Pharmacy
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