Biodistribution of free and encapsulated 99mTc-fluconazole in an infection model induced by Candida albicans

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dc.creatorDanielle Nogueira de Assis
dc.creatorRaquel Silva Araújo
dc.creatorLeonardo Lima Fuscaldi
dc.creatorSimone Odília Antunes Fernandes
dc.creatorVanessa Carla Furtado Mosqueira
dc.creatorValbert Nascimento Cardoso
dc.date.accessioned2022-05-12T21:27:02Z
dc.date.accessioned2025-09-09T01:29:26Z
dc.date.available2022-05-12T21:27:02Z
dc.date.issued2018-03
dc.description.sponsorshipCNPq - Conselho Nacional de Desenvolvimento Científico e Tecnológico
dc.description.sponsorshipFAPEMIG - Fundação de Amparo à Pesquisa do Estado de Minas Gerais
dc.description.sponsorshipCAPES - Coordenação de Aperfeiçoamento de Pessoal de Nível Superior
dc.identifier.doi10.1016/j.biopha.2018.01.021
dc.identifier.issn0753-3322
dc.identifier.urihttps://hdl.handle.net/1843/41627
dc.languageeng
dc.publisherUniversidade Federal de Minas Gerais
dc.relation.ispartofBiomedicine & Pharmacotherapy
dc.rightsAcesso Restrito
dc.subjectCandida albicans
dc.subjectBiodistribuição
dc.subjectTecnécio-99 metaestável
dc.subject.otherInfectious focus
dc.subject.otherBiodistribution
dc.subject.otherNanocapsules
dc.subject.otherTechnetium-99 metastable
dc.subject.otherFluconazole
dc.subject.otherCandida spp
dc.titleBiodistribution of free and encapsulated 99mTc-fluconazole in an infection model induced by Candida albicans
dc.typeArtigo de periódico
local.citation.epage444
local.citation.spage438
local.citation.volume99
local.description.resumoBackground Candida spp is an etiologic agent of fungal infections in hospitals and resistance to treatment with antifungals has been extensively reported. Thus, it is very important to develop formulations that increase effectiveness with low toxicity. In this sense, nanocarriers have been investigated, once they modify drug biodistribution profile. Thus, this study aimed to evaluate the biodistribution of free and encapsulated 99mTc-fluconazole into nanocapsules (NCs) in an experimental immunosuppressed murine model of Candida albicans infection. Methods Fluconazole was radiolabeled with technetium-99 metastable (99mTc) and encapsulated into conventional (99mTc-Fluconazole-PLA-POLOX) and surface-modified (99mTc-Fluconazole-PLA-PEG) NCs by the interfacial deposition of the preformed biodegradable polymer [poly (D,L-lactic acid) (PLA) and PLA–PEG (polyethyleneglycol)] followed by solvent evaporation. The size distribution and zeta potential of the NCs preparations were determined in a Zetasizer by photon correlation spectroscopy and laser Doppler anemometry, respectively. Free and encapsulated 99mTc-fluconazole were administered intravenously in immunosuppressed mice bearing a local infection induced by Candida Albicans inoculation in the right thigh muscle. At pre-established time intervals, tissues and organs of interest were removed and radioactivity was measured in an automatic gamma radiation counter. Results The NCs diameter was between 200 and 400 nm with negative zeta potential values. Free 99mTc-fluconazole was more rapidly eliminated by the renal system compared to the encapsulated drug in NCs, which remained longer in blood circulation. The uptake of conventional NCs by mononuclear phagocyte system organs was higher than the one demonstrated by the surface-modified NCs. Both NCs remained longer in the infectious focus when compared to free 99mTc-fluconazole, but the results did not show a significant difference between NC formulations. Conclusion These data indicate that these NCs might represent a therapeutic alternative for the treatment of candidiasis, once they remain more time in the infectious focus, allowing high retention of 99mTc-fluconazole at this site.
local.publisher.countryBrasil
local.publisher.departmentFAR - DEPARTAMENTO DE ALIMENTOS
local.publisher.departmentFAR - DEPARTAMENTO DE ANÁLISES CLÍNICAS E TOXICOLÓGICAS
local.publisher.initialsUFMG
local.url.externahttps://www.sciencedirect.com/science/article/pii/S0753332217351478?via%3Dihub

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