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

Show simple item record Ramsay, Eva del Amo, Eva M. Toropainen, Elisa Tengvall-Unadike, Unni Ranta, Veli-Pekka Urtti, Arto Ruponen, Marika 2019-04-02T21:56:26Z 2021-12-17T22:02:40Z 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 .
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.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 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.issn 0928-0987
dc.rights.accesslevel openAccess
dc.type.version acceptedVersion

Files in this item

Total number of downloads: Loading...

Files Size Format View
1_s2.0_S0928098718301556_main.pdf 2.235Mb PDF View/Open

This item appears in the following Collection(s)

Show simple item record