Doxorubicin-loaded pH-sensitive micelles: a promising alternative to enhance antitumor activity and reduce toxicity

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dc.creatorCarolina Henriques Cavalcante
dc.creatorAndré Luís Branco de Barros
dc.creatorRenata Salgado Fernandes
dc.creatorJuliana de Oliveira Silva
dc.creatorCaroline Mari Ramos Oda
dc.creatorElaine Amaral Leite
dc.creatorGeovanni Dantas Cassali
dc.creatorIves Charlie Silva
dc.creatorBianca Helena Ventura Fernandes
dc.creatorLucas Antônio Miranda Ferreira
dc.date.accessioned2023-07-17T20:15:55Z
dc.date.accessioned2025-09-09T01:23:25Z
dc.date.available2023-07-17T20:15:55Z
dc.date.issued2021
dc.identifier.doihttps://doi.org/10.1016/j.biopha.2020.111076
dc.identifier.issn0753-3322
dc.identifier.urihttps://hdl.handle.net/1843/56497
dc.languagepor
dc.publisherUniversidade Federal de Minas Gerais
dc.relation.ispartofBiomedicine & Pharmacotherapy
dc.rightsAcesso Aberto
dc.subjectMicelas
dc.subjectDoxorrubicina
dc.subjectDrogas
dc.subject.otherMicelles
dc.subject.otherpH-sensitivity
dc.subject.otherDoxorubicin
dc.subject.otherAntitumor
dc.subject.otherDrug delivery
dc.titleDoxorubicin-loaded pH-sensitive micelles: a promising alternative to enhance antitumor activity and reduce toxicity
dc.typeArtigo de periódico
local.citation.epage11
local.citation.spage1
local.citation.volume134
local.description.resumoDoxorubicin (DOX) is an anthracycline antibiotic widely used in the treatment of cancer, however, it is associated with the occurrence of adverse reactions that limits its clinical use. In this context, the encapsulation of DOX in micelles responsive to pH variations has shown to be a strategy for tumor delivery of the drug, with the potential to increase therapeutic efficacy and to reduce the toxic effects. In addition, radiolabeling nanoparticles with a radioactive isotope is of great use in preclinical studies, since it allows the in vivo monitoring of the nanostructure through the acquisition of quantitative images. Therefore, this study aimed to develop, characterize, and evaluate the antitumor activity of a pH-sensitive micelle composed of DSPE-PEG2000, oleic acid, and DOX. The micelles had a diameter of 13nm, zeta potential near to neutrality, and high encapsulation percentage. The critical micellar concentration (CMC) was 1.4 ×10− 5 mol L-1. The pH-sensitivity was confirmed in vitro through a drug release assay. Cytotoxicity studies confirmed that the encapsulation of DOX into the micelles did not impair the drug cytotoxic activity. Moreover, the incorporation of DSPE-PEG2000-DTPA into the micelles allowed it radiolabeling with the technetium-99m in high yield and stability, permitting its use to monitor antitumor therapy. In this sense, the pH-sensitive micelles were able to inhibit tumor growth significantly when compared to non-pH- sensitive micelles and the free drug. in vivo toxicity evaluation in the zebrafish model revealed significantly lower toxicity of pH-sensitive micelles compared to the free drug. These results indicate that the developed formulation presents itself as a promising alternative to potentiate the treatment of tumors.
local.identifier.orcidhttps://orcid.org/0000-0001-7979-1156
local.identifier.orcidhttps://orcid.org/0000-0002-5214-4407
local.identifier.orcidhttps://orcid.org/0009-0001-0407-1215
local.identifier.orcidhttps://orcid.org/0000-0002-5650-6743
local.identifier.orcidhttps://orcid.org/0000-0002-7572-2767
local.identifier.orcidhttps://orcid.org/0000-0002-2213-4355
local.identifier.orcidhttps://orcid.org/0000-0003-2474-5536
local.publisher.countryBrasil
local.publisher.departmentFAR - DEPARTAMENTO DE ANÁLISES CLÍNICAS E TOXICOLÓGICAS
local.publisher.departmentFAR - DEPARTAMENTO DE PRODUTOS FARMACÊUTICOS
local.publisher.departmentICB - DEPARTAMENTO DE PATOLOGIA
local.publisher.initialsUFMG
local.url.externahttps://www.sciencedirect.com/science/article/pii/S0753332220312695

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