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Inhalable locust bean gum microparticles co-associating isoniazid and rifabutin: therapeutic assessment in a murine model of tuberculosis infection

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Resumo:Tuberculosis is a leading cause of death worldwide. Although the development of new antimycobacterial drugs is an obvious and necessary strategy to address the disease, improving the therapeutic performance of drugs already approved constitutes a valuable alternative approach. As the lung is the most affected organ, where M. tuberculosis is able to survive and proliferate, the direct pulmonary delivery of antitubercular drugs comprises a highly promising therapeutic strategy. In this work, spray-dried locust bean gum (LBG) microparticles were used to deliver a combination of two first line antitubercular drugs, isoniazid (INH) and rifabutin (RFB), to the alveolar zone, where macrophages hosting the bacteria reside. LBG is expected to mediate favoured macrophage uptake of microparticles, leading to enhanced therapeutic effect. The therapeutic effect of LBG/INH/RFB microparticles was evaluated in a murine model infected with M. tuberculosis, strain H37Rv and compared with oral co-therapy of INH and RFB in the free form. The pulmonary administration of LBG/INH/RFB microparticles 5 times per week was the only treatment schedule that provided negative growth index values in lung (-0.22), spleen (-0.14) and liver (-0.26) even using a lower therapeutic dose for both antibiotics. For the control group, the respective values were +1.95, +0.75 and +0.96.
Autores principais:Grenha, Ana
Outros Autores:Alves, Ana D.; Guerreiro, Filipa; Pinho, Jacinta; Simões, Sandra; Almeida, António José; Gaspar, Maria Manuela
Assunto:Tuberculosis Pulmonary delivery Locust bean gum Spray-dried microparticles Rifabutin; isoniazid In vivo studies
Ano:2020
País:Portugal
Tipo de documento:artigo
Tipo de acesso:acesso restrito
Instituição associada:Universidade do Algarve
Idioma:inglês
Origem:Sapientia - Universidade do Algarve
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author Grenha, Ana
author2 Alves, Ana D.
Guerreiro, Filipa
Pinho, Jacinta
Simões, Sandra
Almeida, António José
Gaspar, Maria Manuela
author2_role author
author
author
author
author
author
author_facet Grenha, Ana
Alves, Ana D.
Guerreiro, Filipa
Pinho, Jacinta
Simões, Sandra
Almeida, António José
Gaspar, Maria Manuela
author_role author
contributor_name_str_mv Sapientia
country_str PT
creators_json_txt [{\"Person.name\":\"Grenha, Ana\",\"Person.identifier.orcid\":\"0000-0002-2136-1396\"},{\"Person.name\":\"Alves, Ana D.\"},{\"Person.name\":\"Guerreiro, Filipa\",\"Person.identifier.orcid\":\"0000-0001-6224-1553\"},{\"Person.name\":\"Pinho, Jacinta\"},{\"Person.name\":\"Simões, Sandra\"},{\"Person.name\":\"Almeida, António José\"},{\"Person.name\":\"Gaspar, Maria Manuela\"}]
datacite.contributors.contributor.contributorName.fl_str_mv Sapientia
datacite.creators.creator.creatorName.fl_str_mv Grenha, Ana
Alves, Ana D.
Guerreiro, Filipa
Pinho, Jacinta
Simões, Sandra
Almeida, António José
Gaspar, Maria Manuela
datacite.date.Accepted.fl_str_mv 2020-02-01T00:00:00Z
datacite.date.available.fl_str_mv 2021-02-01T01:30:14Z
datacite.date.embargoed.fl_str_mv 2021-02-01T01:30:14Z
datacite.rights.fl_str_mv http://purl.org/coar/access_right/c_16ec
datacite.subjects.subject.fl_str_mv Tuberculosis
Pulmonary delivery
Locust bean gum
Spray-dried microparticles
Rifabutin; isoniazid
In vivo studies
datacite.titles.title.fl_str_mv Inhalable locust bean gum microparticles co-associating isoniazid and rifabutin: therapeutic assessment in a murine model of tuberculosis infection
dc.contributor.none.fl_str_mv Sapientia
dc.creator.none.fl_str_mv Grenha, Ana
Alves, Ana D.
Guerreiro, Filipa
Pinho, Jacinta
Simões, Sandra
Almeida, António José
Gaspar, Maria Manuela
dc.date.Accepted.fl_str_mv 2020-02-01T00:00:00Z
dc.date.available.fl_str_mv 2021-02-01T01:30:14Z
dc.date.embargoed.fl_str_mv 2021-02-01T01:30:14Z
dc.format.none.fl_str_mv application/pdf
dc.identifier.none.fl_str_mv http://hdl.handle.net/10400.1/13683
dc.language.none.fl_str_mv eng
dc.publisher.none.fl_str_mv Elsevier
dc.rights.none.fl_str_mv http://purl.org/coar/access_right/c_16ec
dc.subject.none.fl_str_mv Tuberculosis
Pulmonary delivery
Locust bean gum
Spray-dried microparticles
Rifabutin; isoniazid
In vivo studies
dc.title.fl_str_mv Inhalable locust bean gum microparticles co-associating isoniazid and rifabutin: therapeutic assessment in a murine model of tuberculosis infection
dc.type.none.fl_str_mv http://purl.org/coar/resource_type/c_6501
description Tuberculosis is a leading cause of death worldwide. Although the development of new antimycobacterial drugs is an obvious and necessary strategy to address the disease, improving the therapeutic performance of drugs already approved constitutes a valuable alternative approach. As the lung is the most affected organ, where M. tuberculosis is able to survive and proliferate, the direct pulmonary delivery of antitubercular drugs comprises a highly promising therapeutic strategy. In this work, spray-dried locust bean gum (LBG) microparticles were used to deliver a combination of two first line antitubercular drugs, isoniazid (INH) and rifabutin (RFB), to the alveolar zone, where macrophages hosting the bacteria reside. LBG is expected to mediate favoured macrophage uptake of microparticles, leading to enhanced therapeutic effect. The therapeutic effect of LBG/INH/RFB microparticles was evaluated in a murine model infected with M. tuberculosis, strain H37Rv and compared with oral co-therapy of INH and RFB in the free form. The pulmonary administration of LBG/INH/RFB microparticles 5 times per week was the only treatment schedule that provided negative growth index values in lung (-0.22), spleen (-0.14) and liver (-0.26) even using a lower therapeutic dose for both antibiotics. For the control group, the respective values were +1.95, +0.75 and +0.96.
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eu_rights_str_mv restrictedAccess
format article
fulltext.url.fl_str_mv https://sapientia.ualg.pt/bitstreams/3fc3f819-2be8-45da-b6ca-0a82b995d39c/download
funding.funder.alternateName_str_mv FCT
FCT
funding.funder.identifier_str_mv http://doi.org/10.13039/501100001871
http://doi.org/10.13039/501100001871
funding.funder.name_str_mv Fundação para a Ciência e a Tecnologia
Fundação para a Ciência e a Tecnologia
funding.name_str_mv 3599-PPCDT
id sapientia_ca6cb2c4610276fa187a5cd9f3bdd9a0
identifier.url.fl_str_mv http://hdl.handle.net/10400.1/13683
instacron_str ualg
institution Universidade do Algarve
instname_str Universidade do Algarve
language eng
network_acronym_str sapientia
network_name_str Sapientia - Universidade do Algarve
oai_identifier_str oai:sapientia.ualg.pt:10400.1/13683
organization_str_mv urn:organizationAcronym:ualg
person_str_mv Grenha, Ana
Grenha, Ana
https://www.ciencia-id.pt/091C-0D58-7225
091C-0D58-7225
http://orcid.org/0000-0002-2136-1396
0000-0002-2136-1396
Alves, Ana D.
Guerreiro, Filipa
Guerreiro, Filipa
https://www.ciencia-id.pt/BF1D-7EFA-19BC
BF1D-7EFA-19BC
http://orcid.org/0000-0001-6224-1553
0000-0001-6224-1553
Pinho, Jacinta
Simões, Sandra
Almeida, António José
Gaspar, Maria Manuela
publishDate 2020
publisher.none.fl_str_mv Elsevier
reponame_str Sapientia - Universidade do Algarve
repository_id_str urn:repositoryAcronym:sapientia
service_str_mv urn:repositoryAcronym:sapientia
spelling engElsevierpt_PTTuberculosis is a leading cause of death worldwide. Although the development of new antimycobacterial drugs is an obvious and necessary strategy to address the disease, improving the therapeutic performance of drugs already approved constitutes a valuable alternative approach. As the lung is the most affected organ, where M. tuberculosis is able to survive and proliferate, the direct pulmonary delivery of antitubercular drugs comprises a highly promising therapeutic strategy. In this work, spray-dried locust bean gum (LBG) microparticles were used to deliver a combination of two first line antitubercular drugs, isoniazid (INH) and rifabutin (RFB), to the alveolar zone, where macrophages hosting the bacteria reside. LBG is expected to mediate favoured macrophage uptake of microparticles, leading to enhanced therapeutic effect. The therapeutic effect of LBG/INH/RFB microparticles was evaluated in a murine model infected with M. tuberculosis, strain H37Rv and compared with oral co-therapy of INH and RFB in the free form. The pulmonary administration of LBG/INH/RFB microparticles 5 times per week was the only treatment schedule that provided negative growth index values in lung (-0.22), spleen (-0.14) and liver (-0.26) even using a lower therapeutic dose for both antibiotics. For the control group, the respective values were +1.95, +0.75 and +0.96.application/pdfpt_PTInhalable locust bean gum microparticles co-associating isoniazid and rifabutin: therapeutic assessment in a murine model of tuberculosis infectionPersonalGrenha, AnaDSpacehttp://dspace.org/items/1bd4d8f1-40e5-45af-b1e8-4b8e73a6a70dDSpacehttp://dspace.org/items/1bd4d8f1-40e5-45af-b1e8-4b8e73a6a70dGrenhaAnaCiência IDhttps://www.ciencia-id.pt091C-0D58-7225ORCIDhttp://orcid.org0000-0002-2136-1396Researcher IDhttps://www.researcherid.comH-1392-2017Scopus Author IDhttps://www.scopus.com8607930100Alves, Ana D.PersonalGuerreiro, FilipaDSpacehttp://dspace.org/items/b88abfe8-e32c-477f-9fb0-5bdeca8a1a05DSpacehttp://dspace.org/items/b88abfe8-e32c-477f-9fb0-5bdeca8a1a05GuerreiroFilipaCiência IDhttps://www.ciencia-id.ptBF1D-7EFA-19BCORCIDhttp://orcid.org0000-0001-6224-1553Pinho, JacintaSimões, SandraAlmeida, António JoséGaspar, Maria ManuelaHostingInstitutionOrganizationalSapientiae-mailmailto:repositorio@ualg.ptrepositorio@ualg.ptISSNIsPartOf0939-6411DOIIsPartOf10.1016/j.ejpb.2019.11.0092021-02-01T01:30:14Z2020-022020-02-01T00:00:00ZHandlehttp://hdl.handle.net/10400.1/13683http://purl.org/coar/access_right/c_16ecrestricted accessTuberculosisPulmonary deliveryLocust bean gumSpray-dried microparticlesRifabutin; isoniazidIn vivo studies550262 bytesFundação para a Ciência e a TecnologiaFighting TB: Development of microparticulate systems to target alveolar macrophages in tuberculosis therapy3599-PPCDTCrossref Funder IDhttp://doi.org/10.13039/501100001871Fundação para a Ciência e a TecnologiaKonjac glucomannan microcarriers: an application in the treatment of pulmonary tuberculosisCrossref Funder IDhttp://doi.org/10.13039/501100001871literaturehttp://purl.org/coar/resource_type/c_6501journal articlehttp://purl.org/coar/access_right/c_16ecapplication/pdffulltexthttps://sapientia.ualg.pt/bitstreams/3fc3f819-2be8-45da-b6ca-0a82b995d39c/downloadEuropean Journal of Pharmaceutics and Biopharmaceutics1473844
spellingShingle Inhalable locust bean gum microparticles co-associating isoniazid and rifabutin: therapeutic assessment in a murine model of tuberculosis infection
Grenha, Ana
Tuberculosis
Pulmonary delivery
Locust bean gum
Spray-dried microparticles
Rifabutin; isoniazid
In vivo studies
status SINGLETON
subject.fl_str_mv Tuberculosis
Pulmonary delivery
Locust bean gum
Spray-dried microparticles
Rifabutin; isoniazid
In vivo studies
title Inhalable locust bean gum microparticles co-associating isoniazid and rifabutin: therapeutic assessment in a murine model of tuberculosis infection
title_full Inhalable locust bean gum microparticles co-associating isoniazid and rifabutin: therapeutic assessment in a murine model of tuberculosis infection
title_fullStr Inhalable locust bean gum microparticles co-associating isoniazid and rifabutin: therapeutic assessment in a murine model of tuberculosis infection
title_full_unstemmed Inhalable locust bean gum microparticles co-associating isoniazid and rifabutin: therapeutic assessment in a murine model of tuberculosis infection
title_short Inhalable locust bean gum microparticles co-associating isoniazid and rifabutin: therapeutic assessment in a murine model of tuberculosis infection
title_sort Inhalable locust bean gum microparticles co-associating isoniazid and rifabutin: therapeutic assessment in a murine model of tuberculosis infection
topic Tuberculosis
Pulmonary delivery
Locust bean gum
Spray-dried microparticles
Rifabutin; isoniazid
In vivo studies
topic_facet Tuberculosis
Pulmonary delivery
Locust bean gum
Spray-dried microparticles
Rifabutin; isoniazid
In vivo studies
url http://hdl.handle.net/10400.1/13683
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