Transport rankings of non-steroidal antiinflammatory drugs across blood-brain barrier in vitro models.

The aim of this work was to conduct a comprehensive study about the transport properties of NSAIDs across the blood-brain barrier (BBB) in vitro. Transport studies with celecoxib, diclofenac, ibuprofen, meloxicam, piroxicam and tenoxicam were accomplished across Transwell models based on cell line P...

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Autores principales:	Iveta Novakova, Eva-Anne Subileau, Stefan Toegel, Daniela Gruber, Bodo Lachmann, Ernst Urban, Christophe Chesne, Christian R Noe, Winfried Neuhaus
Formato:	article
Lenguaje:	EN
Publicado:	Public Library of Science (PLoS) 2014
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/1c4402f3dcbb4e7d97088844741a5b20
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spelling	oai:doaj.org-article:1c4402f3dcbb4e7d97088844741a5b202021-11-18T08:36:03ZTransport rankings of non-steroidal antiinflammatory drugs across blood-brain barrier in vitro models.1932-620310.1371/journal.pone.0086806https://doaj.org/article/1c4402f3dcbb4e7d97088844741a5b202014-01-01T00:00:00Zhttps://www.ncbi.nlm.nih.gov/pmc/articles/pmid/24466249/?tool=EBIhttps://doaj.org/toc/1932-6203The aim of this work was to conduct a comprehensive study about the transport properties of NSAIDs across the blood-brain barrier (BBB) in vitro. Transport studies with celecoxib, diclofenac, ibuprofen, meloxicam, piroxicam and tenoxicam were accomplished across Transwell models based on cell line PBMEC/C1-2, ECV304 or primary rat brain endothelial cells. Single as well as group substance studies were carried out. In group studies substance group compositions, transport medium and serum content were varied, transport inhibitors verapamil and probenecid were added. Resulted permeability coefficients were compared and normalized to internal standards diazepam and carboxyfluorescein. Transport rankings of NSAIDs across each model were obtained. Single substance studies showed similar rankings as corresponding group studies across PBMEC/C1-2 or ECV304 cell layers. Serum content, glioma conditioned medium and inhibitors probenecid and verapamil influenced resulted permeability significantly. Basic differences of transport properties of the investigated NSAIDs were similar comparing all three in vitro BBB models. Different substance combinations in the group studies and addition of probenecid and verapamil suggested that transporter proteins are involved in the transport of every tested NSAID. Results especially underlined the importance of same experimental conditions (transport medium, serum content, species origin, cell line) for proper data comparison.Iveta NovakovaEva-Anne SubileauStefan ToegelDaniela GruberBodo LachmannErnst UrbanChristophe ChesneChristian R NoeWinfried NeuhausPublic Library of Science (PLoS)articleMedicineRScienceQENPLoS ONE, Vol 9, Iss 1, p e86806 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Iveta Novakova Eva-Anne Subileau Stefan Toegel Daniela Gruber Bodo Lachmann Ernst Urban Christophe Chesne Christian R Noe Winfried Neuhaus Transport rankings of non-steroidal antiinflammatory drugs across blood-brain barrier in vitro models.
description	The aim of this work was to conduct a comprehensive study about the transport properties of NSAIDs across the blood-brain barrier (BBB) in vitro. Transport studies with celecoxib, diclofenac, ibuprofen, meloxicam, piroxicam and tenoxicam were accomplished across Transwell models based on cell line PBMEC/C1-2, ECV304 or primary rat brain endothelial cells. Single as well as group substance studies were carried out. In group studies substance group compositions, transport medium and serum content were varied, transport inhibitors verapamil and probenecid were added. Resulted permeability coefficients were compared and normalized to internal standards diazepam and carboxyfluorescein. Transport rankings of NSAIDs across each model were obtained. Single substance studies showed similar rankings as corresponding group studies across PBMEC/C1-2 or ECV304 cell layers. Serum content, glioma conditioned medium and inhibitors probenecid and verapamil influenced resulted permeability significantly. Basic differences of transport properties of the investigated NSAIDs were similar comparing all three in vitro BBB models. Different substance combinations in the group studies and addition of probenecid and verapamil suggested that transporter proteins are involved in the transport of every tested NSAID. Results especially underlined the importance of same experimental conditions (transport medium, serum content, species origin, cell line) for proper data comparison.
format	article
author	Iveta Novakova Eva-Anne Subileau Stefan Toegel Daniela Gruber Bodo Lachmann Ernst Urban Christophe Chesne Christian R Noe Winfried Neuhaus
author_facet	Iveta Novakova Eva-Anne Subileau Stefan Toegel Daniela Gruber Bodo Lachmann Ernst Urban Christophe Chesne Christian R Noe Winfried Neuhaus
author_sort	Iveta Novakova
title	Transport rankings of non-steroidal antiinflammatory drugs across blood-brain barrier in vitro models.
title_short	Transport rankings of non-steroidal antiinflammatory drugs across blood-brain barrier in vitro models.
title_full	Transport rankings of non-steroidal antiinflammatory drugs across blood-brain barrier in vitro models.
title_fullStr	Transport rankings of non-steroidal antiinflammatory drugs across blood-brain barrier in vitro models.
title_full_unstemmed	Transport rankings of non-steroidal antiinflammatory drugs across blood-brain barrier in vitro models.
title_sort	transport rankings of non-steroidal antiinflammatory drugs across blood-brain barrier in vitro models.
publisher	Public Library of Science (PLoS)
publishDate	2014
url	https://doaj.org/article/1c4402f3dcbb4e7d97088844741a5b20
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Transport rankings of non-steroidal antiinflammatory drugs across blood-brain barrier in vitro models.

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