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

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dc.contributor.author Ramsay, Eva
dc.contributor.author del Amo, Eva M.
dc.contributor.author Toropainen, Elisa
dc.contributor.author Tengvall-Unadike, Unni
dc.contributor.author Ranta, Veli-Pekka
dc.contributor.author Urtti, Arto
dc.contributor.author Ruponen, Marika
dc.date.accessioned 2019-04-02T21:56:26Z
dc.date.available 2021-12-17T22:02:40Z
dc.date.issued 2018-07-01
dc.identifier.citation 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
dc.identifier.other PURE: 102952713
dc.identifier.other PURE UUID: f342dd2a-4ed3-423a-993c-02c9417712e7
dc.identifier.other RIS: urn:166271B1049D03BA4A463175B6C94720
dc.identifier.other Scopus: 85045384390
dc.identifier.other WOS: 000432573700009
dc.identifier.uri http://hdl.handle.net/10138/300635
dc.description.abstract 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. en
dc.format.extent 7
dc.language.iso eng
dc.relation.ispartof European Journal of Pharmaceutical Sciences
dc.rights cc_by_nc_nd
dc.rights.uri info:eu-repo/semantics/openAccess
dc.subject Corneal permeability
dc.subject Conjunctival permeability
dc.subject Ocular drug delivery
dc.subject Eye drops
dc.subject Ocular absorption
dc.subject Porcine
dc.subject QSPR
dc.subject TOPICALLY APPLIED PILOCARPINE
dc.subject BETA-BLOCKING-AGENTS
dc.subject QUANTITATIVE-EVALUATION
dc.subject PENETRATION BEHAVIOR
dc.subject PIGMENTED RABBIT
dc.subject ABSORPTION
dc.subject MODEL
dc.subject DELIVERY
dc.subject TIMOLOL
dc.subject SCLERA
dc.subject 317 Pharmacy
dc.title Corneal and conjunctival drug permeability: Systematic comparison and pharmacokinetic impact in the eye en
dc.type Article
dc.contributor.organization Faculty of Pharmacy
dc.contributor.organization Division of Pharmaceutical Biosciences
dc.contributor.organization Drug Research Program
dc.contributor.organization Drug Delivery
dc.contributor.organization Drug Delivery Unit
dc.description.reviewstatus Peer reviewed
dc.relation.doi https://doi.org/10.1016/j.ejps.2018.03.034
dc.relation.issn 0928-0987
dc.rights.accesslevel openAccess
dc.type.version acceptedVersion

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