Corneal and conjunctival drug permeability: Systematic comparison and pharmacokinetic impact in the eye

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Ramsay , E , del Amo , E M , Toropainen , E , Tengvall-Unadike , U , Ranta , V-P , Urtti , A & Ruponen , M 2018 , ' Corneal and conjunctival drug permeability: Systematic comparison and pharmacokinetic impact in the eye ' , European Journal of Pharmaceutical Sciences , vol. 119 , pp. 83-89 . https://doi.org/10.1016/j.ejps.2018.03.034

Titel: Corneal and conjunctival drug permeability: Systematic comparison and pharmacokinetic impact in the eye
Författare: Ramsay, Eva; del Amo, Eva M.; Toropainen, Elisa; Tengvall-Unadike, Unni; Ranta, Veli-Pekka; Urtti, Arto; Ruponen, Marika
Upphovmannens organisation: Faculty of Pharmacy
Division of Pharmaceutical Biosciences
Drug Research Program
Drug Delivery
Drug Delivery Unit
Datum: 2018-07-01
Språk: eng
Sidantal: 7
Tillhör serie: European Journal of Pharmaceutical Sciences
ISSN: 0928-0987
DOI: https://doi.org/10.1016/j.ejps.2018.03.034
Permanenta länken (URI): http://hdl.handle.net/10138/300635
Abstrakt: On the surface of the eye, both the cornea and conjunctiva are restricting ocular absorption of topically applied drugs, but barrier contributions of these two membranes have not been systemically compared. Herein, we studied permeability of 32 small molecular drug compounds across an isolated porcine cornea and built a quantitative structure-property relationship (QSPR) model for the permeability. Corneal drug permeability (data obtained for 25 drug molecules) showed a 52-fold range in permeability (0.09-4.70x10(-6) cm/s) and the most important molecular descriptors in predicting the permeability were hydrogen bond donor, polar surface area and halogen ratio. Corneal permeability values were compared to their conjunctival drug permeability values. Ocular drug bioavailability and systemic absorption via conjunctiva were predicted for this drug set with pharmacokinetic calculations. Drug bioavailability in the aqueous humour was simulated to be <5% and trans-conjunctival systemic absorption was 34-79% of the dose. Loss of drug across the conjunctiva to the blood circulation restricts significantly ocular drug bioavailability and, therefore, ocular absorption does not increase proportionally with the increasing corneal drug permeability.
Subject: Corneal permeability
Conjunctival permeability
Ocular drug delivery
Eye drops
Ocular absorption
Porcine
QSPR
TOPICALLY APPLIED PILOCARPINE
BETA-BLOCKING-AGENTS
QUANTITATIVE-EVALUATION
PENETRATION BEHAVIOR
PIGMENTED RABBIT
ABSORPTION
MODEL
DELIVERY
TIMOLOL
SCLERA
317 Pharmacy
Referentgranskad: Ja
Licens: cc_by_nc_nd
Användningsbegränsning: openAccess
Parallelpublicerad version: acceptedVersion


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