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Engineering of konjac glucomannan into respirable microparticles for delivery of antitubercular drugs

2021Journal article Open Access
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dc.contributor.authorGuerreiro, Filipa
dc.contributor.authorSwedrowska, Magda
dc.contributor.authorPatel, Roshnee
dc.contributor.authorFloréz- Fernández, Noelia
dc.contributor.authorTorres, María Dolores
dc.contributor.authorRosa Da Costa, Ana M.
dc.contributor.authorForbes, Ben
dc.contributor.authorGrenha, Ana
dc.date.accessioned2022-05-09T14:37:59Z
dc.date.available2022-05-09T14:37:59Z
dc.date.issued2021
dc.description.abstractFew medically-approved excipients are available for formulation strategies to endow microcarriers with improved performance in lung drug targeting. Konjac glucomannan (KGM) is a novel, biocompatible material, comprising mannose units potentially inducing macrophage uptake for the treatment of macrophage-mediated diseases. This work investigated spray-dried KGM microparticles as inhalable carriers of model antitubercular drugs, isoniazid (INH) and rifabutin (RFB). The polymer was characterised and different polymer/drug ratios tested in the production of microparticles for which respirability was assessed in vitro. The swelling of KGM microparticles and release of drugs in simulated lung fluid were characterised and the biodegradability in presence of beta-mannosidase, a lung hydrolase, determined. KGM microparticles were drug loaded with 66-91% association efficiency and had aerodynamic diameter around 3 mu m, which enables deep lung penetration. The microparticles swelled upon liquid contact by 40-50% but underwent size reduction (>62% in 90 min) in presence of beta-mannosidase, indicating biodegradability. Finally, drug release was tested showing slower release of RFB compared with INH but complete release of both within 24 h. This work identifies KGM as a biodegradable polymer of natural origin that can be engineered to encapsulate and release drugs in respirable microparticles with physical and chemical macrophage-targeting properties.pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.doi10.1016/j.ijpharm.2021.120731pt_PT
dc.identifier.issn0378-5173
dc.identifier.urihttp://hdl.handle.net/10400.1/17805
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherElsevierpt_PT
dc.relationFighting TB: Development of microparticulate systems to target alveolar macrophages in tuberculosis therapy
dc.relationAlgarve Centre for Marine Sciences
dc.relationKonjac glucomannan microcarriers: an application in the treatment of pulmonary tuberculosis
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/
dc.subjectInhalationpt_PT
dc.subjectKonjac glucomannanpt_PT
dc.subjectMicroparticlespt_PT
dc.subjectPulmonary drug deliverypt_PT
dc.titleEngineering of konjac glucomannan into respirable microparticles for delivery of antitubercular drugspt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.awardTitleFighting TB: Development of microparticulate systems to target alveolar macrophages in tuberculosis therapy
oaire.awardTitleAlgarve Centre for Marine Sciences
oaire.awardTitleKonjac glucomannan microcarriers: an application in the treatment of pulmonary tuberculosis
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/3599-PPCDT/PTDC%2FDTP-FTO%2F0094%2F2012/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB%2F04326%2F2020/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT//SFRH%2FBD%2F115628%2F2016/PT
oaire.citation.startPage120731pt_PT
oaire.citation.titleInternational Journal of Pharmaceuticspt_PT
oaire.citation.volume604pt_PT
oaire.fundingStream3599-PPCDT
oaire.fundingStream6817 - DCRRNI ID
person.familyNameGuerreiro
person.familyNameFlórez-Fernández
person.familyNameRosa da Costa
person.familyNameGrenha
person.givenNameFilipa
person.givenNameNoelia
person.givenNameAna M
person.givenNameAna
person.identifier305029
person.identifier.ciencia-idBF1D-7EFA-19BC
person.identifier.ciencia-idC21E-5E21-0A08
person.identifier.ciencia-idA418-A85E-5DB1
person.identifier.ciencia-id091C-0D58-7225
person.identifier.orcid0000-0001-6224-1553
person.identifier.orcid0000-0002-2666-2315
person.identifier.orcid0000-0003-0225-9537
person.identifier.orcid0000-0002-2136-1396
person.identifier.ridI-1131-2015
person.identifier.ridE-2165-2012
person.identifier.ridH-1392-2017
person.identifier.scopus-author-id57192869367
person.identifier.scopus-author-id53986075100
person.identifier.scopus-author-id8607930100
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.rightsopenAccesspt_PT
rcaap.typearticlept_PT
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