Spray-dried fucoidan microparticles for pulmonary delivery of antitubercular drugs
Autor(a) principal: | |
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Data de Publicação: | 2018 |
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/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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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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1799133270951067648 |