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High Bioavailability of Bisphenol A from Sublingual Exposure

Background: Bisphenol A (BPA) risk assessment is currently hindered by the rejection of reported higher-than-expected plasma BPA concentrations in humans after oral ingestion. These are deemed incompatible with the almost complete hepatic first-pass metabolism of BPA into its inactive glucurono-conj...

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Autores principales: Gayrard, Véronique, Lacroix, Marlène Z., Collet, Séverine H., Viguié, Catherine, Bousquet-Melou, Alain, Toutain, Pierre-Louis, Picard-Hagen, Nicole
Formato: Online Artículo Texto
Lenguaje:English
Publicado: National Institute of Environmental Health Sciences 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3734497/
https://www.ncbi.nlm.nih.gov/pubmed/23761051
http://dx.doi.org/10.1289/ehp.1206339
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author Gayrard, Véronique
Lacroix, Marlène Z.
Collet, Séverine H.
Viguié, Catherine
Bousquet-Melou, Alain
Toutain, Pierre-Louis
Picard-Hagen, Nicole
author_facet Gayrard, Véronique
Lacroix, Marlène Z.
Collet, Séverine H.
Viguié, Catherine
Bousquet-Melou, Alain
Toutain, Pierre-Louis
Picard-Hagen, Nicole
author_sort Gayrard, Véronique
collection PubMed
description Background: Bisphenol A (BPA) risk assessment is currently hindered by the rejection of reported higher-than-expected plasma BPA concentrations in humans after oral ingestion. These are deemed incompatible with the almost complete hepatic first-pass metabolism of BPA into its inactive glucurono-conjugated form, BPA glucuronide (BPAG). Objectives: Using dogs as a valid model, we compared plasma concentrations of BPA over a 24-hr period after intravenous, orogastric, and sublingual administration in order to establish the absolute bioavailability of BPA administered sublingually and to compare it with oral bioavailability. Methods: Six dogs were sublingually administered BPA at 0.05 mg/kg and 5 mg/kg. We compared the time course of plasma BPA concentrations with that obtained in the same dogs after intravenous administration of the same BPA doses and after a 20-mg/kg BPA dose administrated by orogastric gavage. Results: The data indicated that the systemic bioavailability of BPA deposited sublingually was high (70–90%) and that BPA transmucosal absorption from the oral cavity led to much higher BPA internal exposure than obtained for BPA absorption from the gastrointestinal tract. The concentration ratio of BPAG to BPA in plasma was approximately 100-fold lower following sublingual administration than after orogastric dosing, distinguishing the two pathways of absorption. Conclusions: Our findings demonstrate that BPA can be efficiently and very rapidly absorbed through the oral mucosa after sublingual exposure. This efficient systemic entry route of BPA may lead to far higher BPA internal exposures than known for BPA absorption from the gastrointestinal tract.
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spelling pubmed-37344972013-08-07 High Bioavailability of Bisphenol A from Sublingual Exposure Gayrard, Véronique Lacroix, Marlène Z. Collet, Séverine H. Viguié, Catherine Bousquet-Melou, Alain Toutain, Pierre-Louis Picard-Hagen, Nicole Environ Health Perspect Research Background: Bisphenol A (BPA) risk assessment is currently hindered by the rejection of reported higher-than-expected plasma BPA concentrations in humans after oral ingestion. These are deemed incompatible with the almost complete hepatic first-pass metabolism of BPA into its inactive glucurono-conjugated form, BPA glucuronide (BPAG). Objectives: Using dogs as a valid model, we compared plasma concentrations of BPA over a 24-hr period after intravenous, orogastric, and sublingual administration in order to establish the absolute bioavailability of BPA administered sublingually and to compare it with oral bioavailability. Methods: Six dogs were sublingually administered BPA at 0.05 mg/kg and 5 mg/kg. We compared the time course of plasma BPA concentrations with that obtained in the same dogs after intravenous administration of the same BPA doses and after a 20-mg/kg BPA dose administrated by orogastric gavage. Results: The data indicated that the systemic bioavailability of BPA deposited sublingually was high (70–90%) and that BPA transmucosal absorption from the oral cavity led to much higher BPA internal exposure than obtained for BPA absorption from the gastrointestinal tract. The concentration ratio of BPAG to BPA in plasma was approximately 100-fold lower following sublingual administration than after orogastric dosing, distinguishing the two pathways of absorption. Conclusions: Our findings demonstrate that BPA can be efficiently and very rapidly absorbed through the oral mucosa after sublingual exposure. This efficient systemic entry route of BPA may lead to far higher BPA internal exposures than known for BPA absorption from the gastrointestinal tract. National Institute of Environmental Health Sciences 2013-06-12 2013-08 /pmc/articles/PMC3734497/ /pubmed/23761051 http://dx.doi.org/10.1289/ehp.1206339 Text en http://creativecommons.org/publicdomain/mark/1.0/ Publication of EHP lies in the public domain and is therefore without copyright. All text from EHP may be reprinted freely. Use of materials published in EHP should be acknowledged (for example, ?Reproduced with permission from Environmental Health Perspectives?); pertinent reference information should be provided for the article from which the material was reproduced. Articles from EHP, especially the News section, may contain photographs or illustrations copyrighted by other commercial organizations or individuals that may not be used without obtaining prior approval from the holder of the copyright.
spellingShingle Research
Gayrard, Véronique
Lacroix, Marlène Z.
Collet, Séverine H.
Viguié, Catherine
Bousquet-Melou, Alain
Toutain, Pierre-Louis
Picard-Hagen, Nicole
High Bioavailability of Bisphenol A from Sublingual Exposure
title High Bioavailability of Bisphenol A from Sublingual Exposure
title_full High Bioavailability of Bisphenol A from Sublingual Exposure
title_fullStr High Bioavailability of Bisphenol A from Sublingual Exposure
title_full_unstemmed High Bioavailability of Bisphenol A from Sublingual Exposure
title_short High Bioavailability of Bisphenol A from Sublingual Exposure
title_sort high bioavailability of bisphenol a from sublingual exposure
topic Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3734497/
https://www.ncbi.nlm.nih.gov/pubmed/23761051
http://dx.doi.org/10.1289/ehp.1206339
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