Cargando…

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...

Descripción completa

Detalles Bibliográficos
Autores principales: Torrens, Inés, Ganza, Álvaro, Hernández, Gonzalo, Gonzalo, Ana, Zazpe, Arturo
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Mary Ann Liebert, Inc., publishers 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9700334/
https://www.ncbi.nlm.nih.gov/pubmed/36269652
http://dx.doi.org/10.1089/jop.2022.0024
_version_ 1784839288645484544
author Torrens, Inés
Ganza, Álvaro
Hernández, Gonzalo
Gonzalo, Ana
Zazpe, Arturo
author_facet Torrens, Inés
Ganza, Álvaro
Hernández, Gonzalo
Gonzalo, Ana
Zazpe, Arturo
author_sort Torrens, Inés
collection PubMed
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 [C(max): 2,545.04 ng/g, at 6 h postadministration; area under the concentration–time curve (AUC(t)): 11,382.40 ng·h/g] and cornea (C(max): 609.11 ng/g, at 1 h postadministration; AUC(t): 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.
format Online
Article
Text
id pubmed-9700334
institution National Center for Biotechnology Information
language English
publishDate 2022
publisher Mary Ann Liebert, Inc., publishers
record_format MEDLINE/PubMed
spelling pubmed-97003342022-11-30 Ocular Biodistribution of Once-Daily 0.6% Bilastine Eye Drops Reveals Highest Levels in Conjunctiva Up to 24 h Postadministration Torrens, Inés Ganza, Álvaro Hernández, Gonzalo Gonzalo, Ana Zazpe, Arturo J Ocul Pharmacol Ther Original Articles 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 [C(max): 2,545.04 ng/g, at 6 h postadministration; area under the concentration–time curve (AUC(t)): 11,382.40 ng·h/g] and cornea (C(max): 609.11 ng/g, at 1 h postadministration; AUC(t): 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. Mary Ann Liebert, Inc., publishers 2022-11-01 2022-11-08 /pmc/articles/PMC9700334/ /pubmed/36269652 http://dx.doi.org/10.1089/jop.2022.0024 Text en © Inés Torrens et al. 2022; Published by Mary Ann Liebert, Inc. https://creativecommons.org/licenses/by/4.0/This Open Access article is distributed under the terms of the Creative Commons License [CC-BY] (http://creativecommons.org/licenses/by/4.0 (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Original Articles
Torrens, Inés
Ganza, Álvaro
Hernández, Gonzalo
Gonzalo, Ana
Zazpe, Arturo
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
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_short 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
topic Original Articles
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9700334/
https://www.ncbi.nlm.nih.gov/pubmed/36269652
http://dx.doi.org/10.1089/jop.2022.0024
work_keys_str_mv AT torrensines ocularbiodistributionofoncedaily06bilastineeyedropsrevealshighestlevelsinconjunctivaupto24hpostadministration
AT ganzaalvaro ocularbiodistributionofoncedaily06bilastineeyedropsrevealshighestlevelsinconjunctivaupto24hpostadministration
AT hernandezgonzalo ocularbiodistributionofoncedaily06bilastineeyedropsrevealshighestlevelsinconjunctivaupto24hpostadministration
AT gonzaloana ocularbiodistributionofoncedaily06bilastineeyedropsrevealshighestlevelsinconjunctivaupto24hpostadministration
AT zazpearturo ocularbiodistributionofoncedaily06bilastineeyedropsrevealshighestlevelsinconjunctivaupto24hpostadministration