Spray-dried fucoidan microparticles for pulmonary delivery of antitubercular drugs

Detalhes bibliográficos
Autor(a) principal: Cunha, Ludmylla
Data de Publicação: 2018
Outros Autores: Rosa Da Costa, Ana, Lourenço, João P., Buttini, Francesca, Grenha, Ana
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10400.1/12292
Resumo: Pulmonary tuberculosis accounts for 80% of cases and the delivery of antitubercular drugs into the lungs allows targeting the infected organ and, possibly, reducing systemic drug toxicity. This work aimed at using fucoidan as matrix of inhalable microparticles that associate two first-line antitubercular drugs, for an application in pulmonary tuberculosis therapy. Fucoidan is composed of fucose and sulphated sugar residues, moieties described as being recognised by surface receptors of alveolar macrophages, which host mycobacteria. Inhalable fucoidan microparticles loaded with antitubercular drugs were successfully produced with high association efficiencies of either isoniazid (95%) or rifabutin (81%). The microparticles evidenced no cytotoxicity on lung epithelial cells (A549). However, rifabutin-loaded microparticles showed a certain degree of toxicity on macrophage-like cells (THP-1) at the highest tested concentration (1 mg/mL). Furthermore, microparticles showed favourable aerodynamic properties for deep lung delivery (MMAD 2.0-3.8 µm) and, thus, show potential for an application as inhalable tuberculosis therapy.
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spelling Spray-dried fucoidan microparticles for pulmonary delivery of antitubercular drugsA549 cellsAdministrationAntitubercular agentsCell lineDrug carriersDrug liberationHumansIsoniazidPolysaccharidesRifabutinInhalationPulmonary tuberculosis accounts for 80% of cases and the delivery of antitubercular drugs into the lungs allows targeting the infected organ and, possibly, reducing systemic drug toxicity. This work aimed at using fucoidan as matrix of inhalable microparticles that associate two first-line antitubercular drugs, for an application in pulmonary tuberculosis therapy. Fucoidan is composed of fucose and sulphated sugar residues, moieties described as being recognised by surface receptors of alveolar macrophages, which host mycobacteria. Inhalable fucoidan microparticles loaded with antitubercular drugs were successfully produced with high association efficiencies of either isoniazid (95%) or rifabutin (81%). The microparticles evidenced no cytotoxicity on lung epithelial cells (A549). However, rifabutin-loaded microparticles showed a certain degree of toxicity on macrophage-like cells (THP-1) at the highest tested concentration (1 mg/mL). Furthermore, microparticles showed favourable aerodynamic properties for deep lung delivery (MMAD 2.0-3.8 µm) and, thus, show potential for an application as inhalable tuberculosis therapy.Taylor & FrancisSapientiaCunha, LudmyllaRosa Da Costa, AnaLourenço, João P.Buttini, FrancescaGrenha, Ana2019-01-15T16:09:03Z20182018-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10400.1/12292engLudmylla Cunha, Ana M. Rosa da Costa, João P. Lourenço, Francesca Buttini & Ana Grenha (2018) Spray-dried fucoidan microparticles for pulmonary delivery of antitubercular drugs, Journal of Microencapsulation, 35:4, 392-405, DOI: 10.1080/02652048.2018.15130890265-204810.1080/02652048.2018.1513089info: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:RCAAP2023-07-24T10:24:15Zoai:sapientia.ualg.pt:10400.1/12292Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T20:03:38.811430Repositório 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 Spray-dried fucoidan microparticles for pulmonary delivery of antitubercular drugs
title Spray-dried fucoidan microparticles for pulmonary delivery of antitubercular drugs
spellingShingle Spray-dried fucoidan microparticles for pulmonary delivery of antitubercular drugs
Cunha, Ludmylla
A549 cells
Administration
Antitubercular agents
Cell line
Drug carriers
Drug liberation
Humans
Isoniazid
Polysaccharides
Rifabutin
Inhalation
title_short Spray-dried fucoidan microparticles for pulmonary delivery of antitubercular drugs
title_full Spray-dried fucoidan microparticles for pulmonary delivery of antitubercular drugs
title_fullStr Spray-dried fucoidan microparticles for pulmonary delivery of antitubercular drugs
title_full_unstemmed Spray-dried fucoidan microparticles for pulmonary delivery of antitubercular drugs
title_sort Spray-dried fucoidan microparticles for pulmonary delivery of antitubercular drugs
author Cunha, Ludmylla
author_facet Cunha, Ludmylla
Rosa Da Costa, Ana
Lourenço, João P.
Buttini, Francesca
Grenha, Ana
author_role author
author2 Rosa Da Costa, Ana
Lourenço, João P.
Buttini, Francesca
Grenha, Ana
author2_role author
author
author
author
dc.contributor.none.fl_str_mv Sapientia
dc.contributor.author.fl_str_mv Cunha, Ludmylla
Rosa Da Costa, Ana
Lourenço, João P.
Buttini, Francesca
Grenha, Ana
dc.subject.por.fl_str_mv A549 cells
Administration
Antitubercular agents
Cell line
Drug carriers
Drug liberation
Humans
Isoniazid
Polysaccharides
Rifabutin
Inhalation
topic A549 cells
Administration
Antitubercular agents
Cell line
Drug carriers
Drug liberation
Humans
Isoniazid
Polysaccharides
Rifabutin
Inhalation
description Pulmonary tuberculosis accounts for 80% of cases and the delivery of antitubercular drugs into the lungs allows targeting the infected organ and, possibly, reducing systemic drug toxicity. This work aimed at using fucoidan as matrix of inhalable microparticles that associate two first-line antitubercular drugs, for an application in pulmonary tuberculosis therapy. Fucoidan is composed of fucose and sulphated sugar residues, moieties described as being recognised by surface receptors of alveolar macrophages, which host mycobacteria. Inhalable fucoidan microparticles loaded with antitubercular drugs were successfully produced with high association efficiencies of either isoniazid (95%) or rifabutin (81%). The microparticles evidenced no cytotoxicity on lung epithelial cells (A549). However, rifabutin-loaded microparticles showed a certain degree of toxicity on macrophage-like cells (THP-1) at the highest tested concentration (1 mg/mL). Furthermore, microparticles showed favourable aerodynamic properties for deep lung delivery (MMAD 2.0-3.8 µm) and, thus, show potential for an application as inhalable tuberculosis therapy.
publishDate 2018
dc.date.none.fl_str_mv 2018
2018-01-01T00:00:00Z
2019-01-15T16:09:03Z
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/10400.1/12292
url http://hdl.handle.net/10400.1/12292
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Ludmylla Cunha, Ana M. Rosa da Costa, João P. Lourenço, Francesca Buttini & Ana Grenha (2018) Spray-dried fucoidan microparticles for pulmonary delivery of antitubercular drugs, Journal of Microencapsulation, 35:4, 392-405, DOI: 10.1080/02652048.2018.1513089
0265-2048
10.1080/02652048.2018.1513089
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Taylor & Francis
publisher.none.fl_str_mv Taylor & Francis
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
instname_str Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron_str 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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