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Comparison of the Pharmacokinetic Properties of Triamcinolone and Dexamethasone for Local Therapy of the Inner Ear

Some forms of triamcinolone may provide alternate options for local therapy of the inner ear in addition to the steroids currently in use. We compared the perilymph pharmacokinetics of triamcinolone-acetonide, triamcinolone, and dexamethasone, each delivered as crystalline suspensions to guinea pigs...

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Autores principales: Salt, Alec Nicholas, Hartsock, Jared James, Hou, Jennifer, Piu, Fabrice
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6689996/
https://www.ncbi.nlm.nih.gov/pubmed/31427927
http://dx.doi.org/10.3389/fncel.2019.00347
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author Salt, Alec Nicholas
Hartsock, Jared James
Hou, Jennifer
Piu, Fabrice
author_facet Salt, Alec Nicholas
Hartsock, Jared James
Hou, Jennifer
Piu, Fabrice
author_sort Salt, Alec Nicholas
collection PubMed
description Some forms of triamcinolone may provide alternate options for local therapy of the inner ear in addition to the steroids currently in use. We compared the perilymph pharmacokinetics of triamcinolone-acetonide, triamcinolone, and dexamethasone, each delivered as crystalline suspensions to guinea pigs. Triamcinolone-acetonide is a widely used form of the drug with molecular properties that allow it to readily permeate biological barriers. When applied intratympanically triamcinolone-acetonide entered perilymph rapidly but was also found to be eliminated rapidly from perilymph. The rapid rate of elimination severely limits the apical distribution of the drug when applied locally, making it unsuitable for use in the ear. In contrast, triamcinolone, rather than triamcinolone-acetonide, is a more polar form of the molecule, with higher aqueous solubility but calculated to pass less-readily through biological boundaries. Perilymph concentrations generated with intratympanic applications of triamcinolone were comparable to those with triamcinolone-acetonide but elimination measurements showed that triamcinolone was retained in perilymph longer than triamcinolone-acetonide or dexamethasone. The slower elimination is projected to result in improved distribution of triamcinolone toward the cochlear apex, potentially allowing higher drug levels to reach the speech frequency regions of the human ear. These measurements show that triamcinolone could constitute an attractive additional treatment option for local therapy of auditory disorders.
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spelling pubmed-66899962019-08-19 Comparison of the Pharmacokinetic Properties of Triamcinolone and Dexamethasone for Local Therapy of the Inner Ear Salt, Alec Nicholas Hartsock, Jared James Hou, Jennifer Piu, Fabrice Front Cell Neurosci Neuroscience Some forms of triamcinolone may provide alternate options for local therapy of the inner ear in addition to the steroids currently in use. We compared the perilymph pharmacokinetics of triamcinolone-acetonide, triamcinolone, and dexamethasone, each delivered as crystalline suspensions to guinea pigs. Triamcinolone-acetonide is a widely used form of the drug with molecular properties that allow it to readily permeate biological barriers. When applied intratympanically triamcinolone-acetonide entered perilymph rapidly but was also found to be eliminated rapidly from perilymph. The rapid rate of elimination severely limits the apical distribution of the drug when applied locally, making it unsuitable for use in the ear. In contrast, triamcinolone, rather than triamcinolone-acetonide, is a more polar form of the molecule, with higher aqueous solubility but calculated to pass less-readily through biological boundaries. Perilymph concentrations generated with intratympanic applications of triamcinolone were comparable to those with triamcinolone-acetonide but elimination measurements showed that triamcinolone was retained in perilymph longer than triamcinolone-acetonide or dexamethasone. The slower elimination is projected to result in improved distribution of triamcinolone toward the cochlear apex, potentially allowing higher drug levels to reach the speech frequency regions of the human ear. These measurements show that triamcinolone could constitute an attractive additional treatment option for local therapy of auditory disorders. Frontiers Media S.A. 2019-07-30 /pmc/articles/PMC6689996/ /pubmed/31427927 http://dx.doi.org/10.3389/fncel.2019.00347 Text en Copyright © 2019 Salt, Hartsock, Hou and Piu. http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
spellingShingle Neuroscience
Salt, Alec Nicholas
Hartsock, Jared James
Hou, Jennifer
Piu, Fabrice
Comparison of the Pharmacokinetic Properties of Triamcinolone and Dexamethasone for Local Therapy of the Inner Ear
title Comparison of the Pharmacokinetic Properties of Triamcinolone and Dexamethasone for Local Therapy of the Inner Ear
title_full Comparison of the Pharmacokinetic Properties of Triamcinolone and Dexamethasone for Local Therapy of the Inner Ear
title_fullStr Comparison of the Pharmacokinetic Properties of Triamcinolone and Dexamethasone for Local Therapy of the Inner Ear
title_full_unstemmed Comparison of the Pharmacokinetic Properties of Triamcinolone and Dexamethasone for Local Therapy of the Inner Ear
title_short Comparison of the Pharmacokinetic Properties of Triamcinolone and Dexamethasone for Local Therapy of the Inner Ear
title_sort comparison of the pharmacokinetic properties of triamcinolone and dexamethasone for local therapy of the inner ear
topic Neuroscience
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6689996/
https://www.ncbi.nlm.nih.gov/pubmed/31427927
http://dx.doi.org/10.3389/fncel.2019.00347
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