Long-circulating and fusogenic liposomes loaded with a glucoevatromonoside derivative induce potent antitumor response

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dc.creatorEliza Rocha Gomes
dc.creatorRodrigo Maia de Pádua
dc.creatorMônica Cristina de Oliveira
dc.creatorMarcus Novais
dc.creatorIzabella Thaís Silva
dc.creatorAndré Luís Branco de Barros
dc.creatorElaine Amaral Leite
dc.creatorJennifer Munkert
dc.creatorAlessandra Frade
dc.creatorGeovanni Dantas Cassali
dc.creatorFernão Castro Braga
dc.date.accessioned2023-07-17T20:31:28Z
dc.date.accessioned2025-09-09T00:39:16Z
dc.date.available2023-07-17T20:31:28Z
dc.date.issued2018
dc.identifier.doihttps://doi.org/10.1016/j.biopha.2018.09.109
dc.identifier.issn0753-3322
dc.identifier.urihttps://hdl.handle.net/1843/56505
dc.languagepor
dc.publisherUniversidade Federal de Minas Gerais
dc.relation.ispartofBiomedicine & Pharmacotherapy
dc.rightsAcesso Aberto
dc.subjectCâncer de mama
dc.subjectMorte - Causas
dc.subject.otherBreast cancer
dc.subject.otherLung cancer
dc.subject.otherLiposomes
dc.subject.otherCardenolide
dc.subject.otherCytotoxicity
dc.subject.otherAntitumor efficacy
dc.titleLong-circulating and fusogenic liposomes loaded with a glucoevatromonoside derivative induce potent antitumor response
dc.typeArtigo de periódico
local.citation.epage1161
local.citation.spage1152
local.citation.volume108
local.description.resumoCancer is an important public health problem, being one of the leading causes of death worldwide. Most antineoplastic agents cause severe toxic effects and some types of cancer do not respond or are resistant to the existing pharmacotherapy, necessitating the research and development of new therapeutic strategies. CardenolideshaveshownsignificantantitumoractivityduetotheirabilitytoinhibittheNa+K+ATPaseenzyme, and the expression of this enzyme is increased in tumor cells. Glucoevatromonoside containing peracetylated glucose hydroxyl groups (GEVPG) is a cardenolide derivative that has low solubility in aqueous media, which constitutes a barrier to its potential biological applications. In this context, the use of liposomes represents a promising strategy to deliver GEVPG, thus allowing its intravenous administration. In this study, long-circulating and fusogenic liposomes containing GEVPG (SpHL-GEVPG) were developed, and their chemical and physicochemical properties were evaluated. SpHL-GEVPG presented adequate properties, including a mean diameter of182.2 ± 2.7nm,a polydispersity index equalto 0.36 ± 0.03,a zetapotential of–2.37 ± 0.31mV, and a GEVPG entrapment of 0.38 ± 0.04mg/mL. Moreover, this formulation showed a good stability after having been stored for 30 days at 4°C. The cytotoxic studies against breast (MDA-MB-231, MCF-7, and SKBR-3) and lung (A549) cancer cell lines demonstrated that SpHL-GEVPG treatment significantly reduced the cell viability. In addition, the SpHL-GEVPG formulation presented a good selectivity toward these cancer cells. The evaluationofthetherapeuticefficacyofthetreatmentwithSpHL-GEVPGshowedapotentanticancereffectinan A549 human lung cancer xenograft model. SpHL-GEVPG administered at doses of 1.0 and 2.0mg/kg (i.v.) inducedantitumoreffectcomparable topaclitaxelgivenatdoseof10mg/kg(i.v.)tomice.Therefore,theresultsof the present work indicate the potential applicability of SpHL-GEVPG as a new anticancer formulation.
local.identifier.orcidhttps://orcid.org/0000-0003-2773-3063
local.identifier.orcidhttps://orcid.org/0000-0002-9939-6900
local.identifier.orcidhttps://orcid.org/0000-0002-1893-4317
local.identifier.orcidhttps://orcid.org/0000-0001-7979-1156
local.identifier.orcidhttps://orcid.org/0000-0001-8812-3811
local.identifier.orcidhttps://orcid.org/0000-0001-9799-8804
local.identifier.orcidhttps://orcid.org/0000-0003-4607-7495
local.identifier.orcidhttps://orcid.org/0000-0002-5650-6743
local.identifier.orcidhttps://orcid.org/0000-0001-9468-376X
local.publisher.countryBrasil
local.publisher.departmentFAR - DEPARTAMENTO DE PRODUTOS FARMACÊUTICOS
local.publisher.initialsUFMG
local.url.externahttps://www.sciencedirect.com/science/article/pii/S0753332218343439?via%3Dihub

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