Ocular pharmacokinetics of atenolol, timolol and betaxolol cocktail : Tissue exposures in the rabbit eye

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dc.contributor.author Fayyaz, Anam
dc.contributor.author Vellonen, Kati-Sisko
dc.contributor.author Ranta, Veli-Pekka
dc.contributor.author Toropainen, Elisa
dc.contributor.author Reinisalo, Mika
dc.contributor.author Valtari, Annika
dc.contributor.author Puranen, Jooseppi
dc.contributor.author Ricci, Giuseppe D'Amico
dc.contributor.author Heikkinen, Emma M.
dc.contributor.author Gardner, Iain
dc.contributor.author Ruponen, Marika
dc.contributor.author Urtti, Arto
dc.contributor.author Jamei, Masoud
dc.contributor.author Amo, Eva M. del
dc.date.accessioned 2021-08-12T12:08:11Z
dc.date.available 2021-08-12T12:08:11Z
dc.date.issued 2021-09
dc.identifier.citation Fayyaz , A , Vellonen , K-S , Ranta , V-P , Toropainen , E , Reinisalo , M , Valtari , A , Puranen , J , Ricci , G DA , Heikkinen , E M , Gardner , I , Ruponen , M , Urtti , A , Jamei , M & Amo , E M D 2021 , ' Ocular pharmacokinetics of atenolol, timolol and betaxolol cocktail : Tissue exposures in the rabbit eye ' , European Journal of Pharmaceutics and Biopharmaceutics , vol. 166 , pp. 155-162 . https://doi.org/10.1016/j.ejpb.2021.06.003
dc.identifier.other PURE: 167433137
dc.identifier.other PURE UUID: 979a10d9-fa7d-4f80-9f84-e516f7322eb8
dc.identifier.other WOS: 000678362200006
dc.identifier.uri http://hdl.handle.net/10138/333103
dc.description.abstract Quantitative understanding of pharmacokinetics of topically applied ocular drugs requires more research to further understanding and to eventually allow predictive in silico models to be developed. To this end, a topical cocktail of betaxolol, timolol and atenolol was instilled on albino rabbit eyes. Tear fluid, corneal epithelium, corneal stroma with endothelium, bulbar conjunctiva, anterior sclera, iris-ciliary body, lens and vitreous samples were collected and analysed using LC-MS/MS. Iris-ciliary body was also analysed after intracameral cocktail injection. Non-compartmental analysis was utilized to estimate the pharmacokinetics parameters. The most lipophilic drug, betaxolol, presented the highest exposure in all tissues except for tear fluid after topical administration, followed by timolol and atenolol. For all drugs, iris-ciliary body concentrations were higher than that of the aqueous humor. After topical instillation the most hydrophilic drug, atenolol, had 3.7 times higher AUCiris-ciliary body than AUCaqueous humor, whereas the difference was 1.4 and 1.6 times for timolol and betaxolol, respectively. This suggests that the non-corneal route (conjunctival-scleral) was dominating the absorption of atenolol, while the corneal route was more important for timolol and betaxolol. The presented data increase understanding of ocular pharmacokinetics of a cocktail of drugs and provide data that can be used for quantitative modeling and simulation. en
dc.format.extent 8
dc.language.iso eng
dc.relation.ispartof European Journal of Pharmaceutics and Biopharmaceutics
dc.rights cc_by
dc.rights.uri info:eu-repo/semantics/openAccess
dc.subject Timolol
dc.subject Betaxolol
dc.subject Atenolol
dc.subject Ocular pharmacokinetics
dc.subject Rabbit
dc.subject Topical
dc.subject Intracameral
dc.subject Corneal route
dc.subject Conjunctival-scleral route
dc.subject BETA-BLOCKERS
dc.subject PILOCARPINE
dc.subject CORNEAL
dc.subject FLUORESCEIN
dc.subject CLEARANCE
dc.subject 317 Pharmacy
dc.title Ocular pharmacokinetics of atenolol, timolol and betaxolol cocktail : Tissue exposures in the rabbit eye en
dc.type Article
dc.contributor.organization Drug Research Program
dc.contributor.organization Drug Delivery
dc.contributor.organization Drug Delivery Unit
dc.contributor.organization Division of Pharmaceutical Biosciences
dc.description.reviewstatus Peer reviewed
dc.relation.doi https://doi.org/10.1016/j.ejpb.2021.06.003
dc.relation.issn 0939-6411
dc.rights.accesslevel openAccess
dc.type.version publishedVersion

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