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Radiolabeled block copolymer micelles for image-guided drug delivery

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dc.contributor.authorRibeiro, Elisabete
dc.contributor.authorAlho, Irina
dc.contributor.authorMarques, Fernanda
dc.contributor.authorGano, Lurdes
dc.contributor.authorCorreia, Isabel
dc.contributor.authorCorreia, João D. G.
dc.contributor.authorCasimiro, Sandra
dc.contributor.authorCosta, Luis
dc.contributor.authorSantos, Isabel Cordeiro
dc.contributor.authorFernandes, Célia
dc.date.accessioned2022-02-21T17:44:24Z
dc.date.available2022-02-21T17:44:24Z
dc.date.issued2016
dc.description© 2016 Elsevier B.V. All rights reservedpt_PT
dc.description.abstractWe aimed at exploring block copolymer micelles (BCMs) for the simultaneous delivery of radiation/chemotherapy to cancer cells. To achieve that goal, we have prepared and characterized a novel type of docetaxel (DTX) loaded and non-loaded BCMs. The micelles were decorated with pyrazolyl-diamine chelating units to stabilize the matched pair 99mTc/Re for image-guided delivery of therapeutic drugs. The in vitro studies have shown that DTX release is pH-dependent increasing at lower pH values. Anti-proliferative studies in different cancer cell lines showed that DTX-loaded BCMs present relevant anti-proliferative activity. In comparison to free DTX, the loaded-micelles exhibited higher anti-proliferative activity for the same DTX concentration, which mean that a similar therapeutic outcome may be achieved with reduced side effects. The pyrazolyl-diamine-functionalized micelles were labeled with fac-[99mTc(CO)3(H2O)3]+ in high radiochemical yield and purity. The radiolabeled micelles are stable in phosphate buffer and in cell culture media. Cellular uptake studies in different cancer cell lines indicate a cell type and time-dependent uptake, in agreement with the anti-proliferative activity. Early biodistribution studies in healthy BALB/c mice has shown prolonged circulation lifetime in the bloodstream and relevant in vivo stability, important features when considering an effective DTX delivery system and image-guided delivery agent for cancer theranostics.pt_PT
dc.description.sponsorshipThis research was supported by the Fundação para a Ciência e Tecnologia (FCT) through the project EXCL/QEQ-MED/0233/2012 and carried out within European COST actions TD1004. C2TN/IST authors gratefully acknowledge the FCT support through the UID/Multi/04349/2013 project. Elisabete Ribeiro acknowledges the FCT research grant.pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.citationInternational Journal of Pharmaceutics 515 (2016) 692–701pt_PT
dc.identifier.doi10.1016/j.ijpharm.2016.11.004pt_PT
dc.identifier.eissn1873-3476
dc.identifier.issn0378-5173
dc.identifier.urihttp://hdl.handle.net/10451/51440
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherElsevierpt_PT
dc.relation.publisherversionhttps://www.sciencedirect.com/journal/international-journal-of-pharmaceuticspt_PT
dc.subject(99m)Tcpt_PT
dc.subjectBlock copolymer micellept_PT
dc.subjectDrug delivery systempt_PT
dc.subjectPEG-b-PCLpt_PT
dc.subjectRadiolabeled micellespt_PT
dc.titleRadiolabeled block copolymer micelles for image-guided drug deliverypt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/3599-PPCDT/EXCL%2FQEQ-MED%2F0233%2F2012/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/5876/UID%2FMulti%2F04349%2F2013/PT
oaire.citation.endPage701pt_PT
oaire.citation.issue1-2pt_PT
oaire.citation.startPage692pt_PT
oaire.citation.titleInternational Journal of Pharmaceuticspt_PT
oaire.citation.volume515pt_PT
oaire.fundingStream3599-PPCDT
oaire.fundingStream5876
person.familyNameRibeiro
person.familyNameDuarte
person.familyNameMarujo Marques
person.familyNameBarrela Patricio Gano
person.familyNameCorreia
person.familyNameCorreia
person.familyNameCara de Anjo Casimiro
person.familyNameCosta
person.familyNameCordeiro Santos
person.familyNameFernandes
person.givenNameElisabete
person.givenNameIrina
person.givenNameFernanda
person.givenNameMaria Lurdes
person.givenNameIsabel
person.givenNameJoão
person.givenNameSandra Cristina
person.givenNameLuis
person.givenNameIsabel
person.givenNameCélia
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person.identifier.ridA-9552-2015
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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.rightsrestrictedAccesspt_PT
rcaap.typearticlept_PT
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