Intranasal administration of carbamazepine to mice: a direct delivery pathway for brain targeting
Autor(a) principal: | |
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Data de Publicação: | 2014 |
Outros Autores: | , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
Texto Completo: | http://hdl.handle.net/10316/27918 https://doi.org/10.1016/j.ejps.2014.04.019 |
Resumo: | The currently available antiepileptic drugs are typically administered via oral or intravenous (IV) routes which commonly exhibit high systemic distribution into non-targeted tissues, leading to peripheral adverse effects and limited brain uptake. In order to improve the efficacy and tolerability of the antiepileptic drug therapy, alternative administration strategies have been investigated. The purpose of the present study was to assess the pharmacokinetics of carbamazepine administered via intranasal (IN) and IV routes to mice, and to investigate whether a direct transport of the drug from nose to brain could be involved. The similar pharmacokinetic profiles obtained in all matrices following both administration routes indicate that, after IN delivery, carbamazepine reaches quickly and extensively the bloodstream, achieving the brain predominantly via systemic circulation. However, the uneven biodistribution of carbamazepine through the brain regions with higher concentrations in the olfactory bulb and frontal cortex following IN instillation, in comparison with the homogenous brain distribution pattern after IV injection, strongly suggests the involvement of a direct transport of carbamazepine from nose to brain. Therefore, it seems that IN delivery represents a suitable and promising alternative route to administer carbamazepine not only for the chronically use of the drug but also in emergency conditions. |
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Intranasal administration of carbamazepine to mice: a direct delivery pathway for brain targetingCarbamazepineIntranasal administrationPharmacokineticsNose-to-brain drug deliveryBrain distributionMiceThe currently available antiepileptic drugs are typically administered via oral or intravenous (IV) routes which commonly exhibit high systemic distribution into non-targeted tissues, leading to peripheral adverse effects and limited brain uptake. In order to improve the efficacy and tolerability of the antiepileptic drug therapy, alternative administration strategies have been investigated. The purpose of the present study was to assess the pharmacokinetics of carbamazepine administered via intranasal (IN) and IV routes to mice, and to investigate whether a direct transport of the drug from nose to brain could be involved. The similar pharmacokinetic profiles obtained in all matrices following both administration routes indicate that, after IN delivery, carbamazepine reaches quickly and extensively the bloodstream, achieving the brain predominantly via systemic circulation. However, the uneven biodistribution of carbamazepine through the brain regions with higher concentrations in the olfactory bulb and frontal cortex following IN instillation, in comparison with the homogenous brain distribution pattern after IV injection, strongly suggests the involvement of a direct transport of carbamazepine from nose to brain. Therefore, it seems that IN delivery represents a suitable and promising alternative route to administer carbamazepine not only for the chronically use of the drug but also in emergency conditions.Elsevier2014-08-18info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://hdl.handle.net/10316/27918http://hdl.handle.net/10316/27918https://doi.org/10.1016/j.ejps.2014.04.019engSERRALHEIRO, Ana [et. al] - Intranasal administration of carbamazepine to mice: a direct delivery pathway for brain targeting. "European Journal of Pharmaceutical Sciences". ISSN 0928-0987. Vol. 60 (2014) p. 32–390928-0987http://www.sciencedirect.com/science/article/pii/S0928098714001833Serralheiro, AnaAlves, GilbertoFortuna, AnaFalcão, Amílcarinfo:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2020-05-29T09:42:27Zoai:estudogeral.uc.pt:10316/27918Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T20:53:37.192108Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse |
dc.title.none.fl_str_mv |
Intranasal administration of carbamazepine to mice: a direct delivery pathway for brain targeting |
title |
Intranasal administration of carbamazepine to mice: a direct delivery pathway for brain targeting |
spellingShingle |
Intranasal administration of carbamazepine to mice: a direct delivery pathway for brain targeting Serralheiro, Ana Carbamazepine Intranasal administration Pharmacokinetics Nose-to-brain drug delivery Brain distribution Mice |
title_short |
Intranasal administration of carbamazepine to mice: a direct delivery pathway for brain targeting |
title_full |
Intranasal administration of carbamazepine to mice: a direct delivery pathway for brain targeting |
title_fullStr |
Intranasal administration of carbamazepine to mice: a direct delivery pathway for brain targeting |
title_full_unstemmed |
Intranasal administration of carbamazepine to mice: a direct delivery pathway for brain targeting |
title_sort |
Intranasal administration of carbamazepine to mice: a direct delivery pathway for brain targeting |
author |
Serralheiro, Ana |
author_facet |
Serralheiro, Ana Alves, Gilberto Fortuna, Ana Falcão, Amílcar |
author_role |
author |
author2 |
Alves, Gilberto Fortuna, Ana Falcão, Amílcar |
author2_role |
author author author |
dc.contributor.author.fl_str_mv |
Serralheiro, Ana Alves, Gilberto Fortuna, Ana Falcão, Amílcar |
dc.subject.por.fl_str_mv |
Carbamazepine Intranasal administration Pharmacokinetics Nose-to-brain drug delivery Brain distribution Mice |
topic |
Carbamazepine Intranasal administration Pharmacokinetics Nose-to-brain drug delivery Brain distribution Mice |
description |
The currently available antiepileptic drugs are typically administered via oral or intravenous (IV) routes which commonly exhibit high systemic distribution into non-targeted tissues, leading to peripheral adverse effects and limited brain uptake. In order to improve the efficacy and tolerability of the antiepileptic drug therapy, alternative administration strategies have been investigated. The purpose of the present study was to assess the pharmacokinetics of carbamazepine administered via intranasal (IN) and IV routes to mice, and to investigate whether a direct transport of the drug from nose to brain could be involved. The similar pharmacokinetic profiles obtained in all matrices following both administration routes indicate that, after IN delivery, carbamazepine reaches quickly and extensively the bloodstream, achieving the brain predominantly via systemic circulation. However, the uneven biodistribution of carbamazepine through the brain regions with higher concentrations in the olfactory bulb and frontal cortex following IN instillation, in comparison with the homogenous brain distribution pattern after IV injection, strongly suggests the involvement of a direct transport of carbamazepine from nose to brain. Therefore, it seems that IN delivery represents a suitable and promising alternative route to administer carbamazepine not only for the chronically use of the drug but also in emergency conditions. |
publishDate |
2014 |
dc.date.none.fl_str_mv |
2014-08-18 |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://hdl.handle.net/10316/27918 http://hdl.handle.net/10316/27918 https://doi.org/10.1016/j.ejps.2014.04.019 |
url |
http://hdl.handle.net/10316/27918 https://doi.org/10.1016/j.ejps.2014.04.019 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
SERRALHEIRO, Ana [et. al] - Intranasal administration of carbamazepine to mice: a direct delivery pathway for brain targeting. "European Journal of Pharmaceutical Sciences". ISSN 0928-0987. Vol. 60 (2014) p. 32–39 0928-0987 http://www.sciencedirect.com/science/article/pii/S0928098714001833 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.publisher.none.fl_str_mv |
Elsevier |
publisher.none.fl_str_mv |
Elsevier |
dc.source.none.fl_str_mv |
reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação instacron:RCAAP |
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Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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RCAAP |
institution |
RCAAP |
reponame_str |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
collection |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
repository.name.fl_str_mv |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
repository.mail.fl_str_mv |
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1799133822884773888 |