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Inhalable spray-dried chondroitin sulphate microparticles: effect of different solvents on particle properties and drug activity

2020-02-12Journal article Open access
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dc.contributor.authorRodrigues, Susana
dc.contributor.authorda Costa, Ana M Rosa
dc.contributor.authorFlórez Fernández, Noelia
dc.contributor.authorTorres, María Dolores
dc.contributor.authorFaleiro, Maria Leonor
dc.contributor.authorButtini, Francesca
dc.contributor.authorGrenha, Ana
dc.date.accessioned2020-04-03T10:37:40Z
dc.date.available2020-04-03T10:37:40Z
dc.date.issued2020-02-12
dc.description.abstractSpray-drying stands as one of the most used techniques to produce inhalable microparticles, but several parameters from both the process and the used materials affect the properties of the resulting microparticles. In this work, we describe the production of drug-loaded chondroitin sulphate microparticles by spray-drying, testing the effect of using different solvents during the process. Full characterisation of the polymer and of the aerodynamic properties of the obtained microparticles are provided envisaging an application in inhalable tuberculosis therapy. The spray-dried microparticles successfully associated two first-line antitubercular drugs (isoniazid and rifabutin) with satisfactory production yield (up to 85%) and drug association efficiency (60%-95%). Ethanol and HCl were tested as co-solvents to aid the solubilisation of rifabutin and microparticles produced with the former generally revealed the best features, presenting a better ability to sustainably release rifabutin. Moreover, these presented aerodynamic properties compatible with deep lung deposition, with an aerodynamic diameter around 4 μm and fine particle fraction of approximately 44%. Finally, it was further demonstrated that the antitubercular activity of the drugs remained unchanged after encapsulation independently of the used solvent.pt_PT
dc.description.sponsorshipUID/Multi/04326/2019; SFRH/BD/52426/2013; ED481B 2018/071pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.doi10.3390/polym12020425pt_PT
dc.identifier.issn2073-4360
dc.identifier.urihttp://hdl.handle.net/10400.1/13686
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherMDPIpt_PT
dc.relationFighting TB: Development of microparticulate systems to target alveolar macrophages in tuberculosis therapy
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/pt_PT
dc.subjectChondroitin sulfatept_PT
dc.subjectIsoniazidpt_PT
dc.subjectInhalable microparticlespt_PT
dc.subjectRifabutinpt_PT
dc.subjectSolventspt_PT
dc.subjectSpray-dryingpt_PT
dc.titleInhalable spray-dried chondroitin sulphate microparticles: effect of different solvents on particle properties and drug activitypt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.awardTitleFighting TB: Development of microparticulate systems to target alveolar macrophages in tuberculosis therapy
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/3599-PPCDT/PTDC%2FDTP-FTO%2F0094%2F2012/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/5876/UID%2FBIM%2F04773%2F2013/PT
oaire.citation.issue2pt_PT
oaire.citation.titlePolymerspt_PT
oaire.citation.volume12pt_PT
oaire.fundingStream3599-PPCDT
oaire.fundingStream5876
person.familyNameRodrigues
person.familyNameFaleiro
person.familyNameGrenha
person.givenNameSusana
person.givenNameMaria Leonor
person.givenNameAna
person.identifier252666
person.identifier.ciencia-id9D1A-6537-0383
person.identifier.ciencia-id281D-5E01-F09A
person.identifier.ciencia-id091C-0D58-7225
person.identifier.orcid0000-0002-0329-4265
person.identifier.orcid0000-0002-3878-6948
person.identifier.orcid0000-0002-2136-1396
person.identifier.ridH-1392-2017
person.identifier.scopus-author-id55125292100
person.identifier.scopus-author-id6507927018
person.identifier.scopus-author-id8607930100
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
rcaap.rightsopenAccesspt_PT
rcaap.typearticlept_PT
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