Ocular Biodistribution of Once-Daily 0.6% Bilastine Eye Drops Reveals Highest Levels in Conjunctiva Up to 24 h Postadministration

Purpose: Bilastine is a second-generation antihistamine that has been shown to be effective for treatment of allergic conjunctivitis. The objective of this study was to evaluate the pharmacokinetics (PKs) and biodistribution of 0.6% bilastine preservative-free eye drops. Methods: Bilastine was quant...

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Autores: Torrens, Inés, Ganza, Álvaro, Hernández, Gonzalo, Gonzalo, Ana, Zazpe, Arturo
Formato: artículo
Fecha de publicación:2022
País:España
Recursos:TECNALIA Research & Innovation
Repositorio:TECNALIA Publications
Idioma:inglés
OAI Identifier:oai:dsp.tecnalia.com:11556/5346
Acesso em linha:https://hdl.handle.net/11556/5346
Access Level:acceso abierto
Palavra-chave:allergic conjunctivitis
antihistamines
bilastine
biodistribution
LC-MS/MS
pharmacokinetics
Ophthalmology
Pharmacology
Pharmacology (medical)
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spelling Ocular Biodistribution of Once-Daily 0.6% Bilastine Eye Drops Reveals Highest Levels in Conjunctiva Up to 24 h PostadministrationTorrens, InésGanza, ÁlvaroHernández, GonzaloGonzalo, AnaZazpe, Arturoallergic conjunctivitisantihistaminesbilastinebiodistributionLC-MS/MSpharmacokineticsOphthalmologyPharmacologyPharmacology (medical)Purpose: Bilastine is a second-generation antihistamine that has been shown to be effective for treatment of allergic conjunctivitis. The objective of this study was to evaluate the pharmacokinetics (PKs) and biodistribution of 0.6% bilastine preservative-free eye drops. Methods: Bilastine was quantified in the conjunctiva, cornea, aqueous humor, vitreous humor, iris/ciliary body, retina/choroid, crystalline lens, and plasma, following a single topical administration to male Dutch-belted rabbits. Results: Concentrations of bilastine were highest in the conjunctiva [Cmax: 2,545.04 ng/g, at 6 h postadministration; area under the concentration-time curve (AUCt): 11,382.40 ng·h/g] and cornea (Cmax: 609.11 ng/g, at 1 h postadministration; AUCt: 1,993.88 ng·h/g), followed by the iris/ciliary body, retina/choroid, aqueous humor, plasma, vitreous humor, and crystalline lens. Quantifiable bilastine concentrations were observed up to 24 h after instillation in the conjunctiva (388.45 ng/g), cornea (28.68 ng/g), iris/ciliary body (12.42 ng/g), retina/choroid (1.91 ng/g), and crystalline lens (0.12 ng/g). In plasma, aqueous humor, and vitreous humor, bilastine was detected up to 12 h postadministration (0.18 ng/mL, 0.40 ng/mL, and 0.32 ng/g, respectively). Conclusions: PKs and biodistribution of 0.6% bilastine eye drops in rabbits revealed a marked preferential distribution in the conjunctiva (target tissue), with sustained levels up to 24 h. These findings are consistent with clinical efficacy trials supporting once-daily administration of topical bilastine for treatment of allergic conjunctivitis.Centros PRE-FUSION TECNALIA - (FORMER)20242024-09-1320222022-11-0120222022-11-01journal articlehttp://purl.org/coar/resource_type/c_6501info:eu-repo/semantics/articlehttps://hdl.handle.net/11556/5346reponame:TECNALIA Publicationsinstname:TECNALIA Research & InnovationInglésengopen accesshttp://purl.org/coar/access_right/c_abf2info:eu-repo/semantics/openAccessoai:dsp.tecnalia.com:11556/53462026-06-12T12:42:27Z
dc.title.none.fl_str_mv Ocular Biodistribution of Once-Daily 0.6% Bilastine Eye Drops Reveals Highest Levels in Conjunctiva Up to 24 h Postadministration
title Ocular Biodistribution of Once-Daily 0.6% Bilastine Eye Drops Reveals Highest Levels in Conjunctiva Up to 24 h Postadministration
spellingShingle Ocular Biodistribution of Once-Daily 0.6% Bilastine Eye Drops Reveals Highest Levels in Conjunctiva Up to 24 h Postadministration
Torrens, Inés
allergic conjunctivitis
antihistamines
bilastine
biodistribution
LC-MS/MS
pharmacokinetics
Ophthalmology
Pharmacology
Pharmacology (medical)
title_short Ocular Biodistribution of Once-Daily 0.6% Bilastine Eye Drops Reveals Highest Levels in Conjunctiva Up to 24 h Postadministration
title_full Ocular Biodistribution of Once-Daily 0.6% Bilastine Eye Drops Reveals Highest Levels in Conjunctiva Up to 24 h Postadministration
title_fullStr Ocular Biodistribution of Once-Daily 0.6% Bilastine Eye Drops Reveals Highest Levels in Conjunctiva Up to 24 h Postadministration
title_full_unstemmed Ocular Biodistribution of Once-Daily 0.6% Bilastine Eye Drops Reveals Highest Levels in Conjunctiva Up to 24 h Postadministration
title_sort Ocular Biodistribution of Once-Daily 0.6% Bilastine Eye Drops Reveals Highest Levels in Conjunctiva Up to 24 h Postadministration
dc.creator.none.fl_str_mv Torrens, Inés
Ganza, Álvaro
Hernández, Gonzalo
Gonzalo, Ana
Zazpe, Arturo
author Torrens, Inés
author_facet Torrens, Inés
Ganza, Álvaro
Hernández, Gonzalo
Gonzalo, Ana
Zazpe, Arturo
author_role author
author2 Ganza, Álvaro
Hernández, Gonzalo
Gonzalo, Ana
Zazpe, Arturo
author2_role author
author
author
author
dc.contributor.none.fl_str_mv Centros PRE-FUSION TECNALIA - (FORMER)
dc.subject.none.fl_str_mv allergic conjunctivitis
antihistamines
bilastine
biodistribution
LC-MS/MS
pharmacokinetics
Ophthalmology
Pharmacology
Pharmacology (medical)
topic allergic conjunctivitis
antihistamines
bilastine
biodistribution
LC-MS/MS
pharmacokinetics
Ophthalmology
Pharmacology
Pharmacology (medical)
description Purpose: Bilastine is a second-generation antihistamine that has been shown to be effective for treatment of allergic conjunctivitis. The objective of this study was to evaluate the pharmacokinetics (PKs) and biodistribution of 0.6% bilastine preservative-free eye drops. Methods: Bilastine was quantified in the conjunctiva, cornea, aqueous humor, vitreous humor, iris/ciliary body, retina/choroid, crystalline lens, and plasma, following a single topical administration to male Dutch-belted rabbits. Results: Concentrations of bilastine were highest in the conjunctiva [Cmax: 2,545.04 ng/g, at 6 h postadministration; area under the concentration-time curve (AUCt): 11,382.40 ng·h/g] and cornea (Cmax: 609.11 ng/g, at 1 h postadministration; AUCt: 1,993.88 ng·h/g), followed by the iris/ciliary body, retina/choroid, aqueous humor, plasma, vitreous humor, and crystalline lens. Quantifiable bilastine concentrations were observed up to 24 h after instillation in the conjunctiva (388.45 ng/g), cornea (28.68 ng/g), iris/ciliary body (12.42 ng/g), retina/choroid (1.91 ng/g), and crystalline lens (0.12 ng/g). In plasma, aqueous humor, and vitreous humor, bilastine was detected up to 12 h postadministration (0.18 ng/mL, 0.40 ng/mL, and 0.32 ng/g, respectively). Conclusions: PKs and biodistribution of 0.6% bilastine eye drops in rabbits revealed a marked preferential distribution in the conjunctiva (target tissue), with sustained levels up to 24 h. These findings are consistent with clinical efficacy trials supporting once-daily administration of topical bilastine for treatment of allergic conjunctivitis.
publishDate 2022
dc.date.none.fl_str_mv 2022
2022-11-01
2022
2022-11-01
2024
2024-09-13
dc.type.none.fl_str_mv journal article
http://purl.org/coar/resource_type/c_6501
dc.type.openaire.fl_str_mv info:eu-repo/semantics/article
format article
dc.identifier.none.fl_str_mv https://hdl.handle.net/11556/5346
url https://hdl.handle.net/11556/5346
dc.language.none.fl_str_mv Inglés
eng
language_invalid_str_mv Inglés
language eng
dc.rights.none.fl_str_mv open access
http://purl.org/coar/access_right/c_abf2
dc.rights.openaire.fl_str_mv info:eu-repo/semantics/openAccess
rights_invalid_str_mv open access
http://purl.org/coar/access_right/c_abf2
eu_rights_str_mv openAccess
dc.source.none.fl_str_mv reponame:TECNALIA Publications
instname:TECNALIA Research & Innovation
instname_str TECNALIA Research & Innovation
reponame_str TECNALIA Publications
collection TECNALIA Publications
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15,812429

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