Encapsulation of benznidazole in nanostructured lipid carriers and increased trypanocidal activity in a resistant Trypanosoma cruzi strain

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dc.creatorFlávia Lidiane Oliveira Da Silva
dc.creatorMaria Betânia de Freitas Marques
dc.creatorMaria Irene Yoshida
dc.creatorWagner da Nova Mussel
dc.creatorJoão Vinícios Wirbitzki da Silveira
dc.creatorPoliana Ribeiro Barroso
dc.creatorKelly Cristina Kato
dc.creatorHelen Rodrigues Martins
dc.creatorGuilherme Carneiro
dc.date.accessioned2025-09-03T12:02:10Z
dc.date.accessioned2025-09-09T01:20:46Z
dc.date.available2025-09-03T12:02:10Z
dc.date.issued2023
dc.description.sponsorshipFAPEMIG - Fundação de Amparo à Pesquisa do Estado de Minas Gerais
dc.format.mimetypepdf
dc.identifier.doi10.1590/s2175-97902023e22111
dc.identifier.issn21759790
dc.identifier.urihttps://hdl.handle.net/1843/84801
dc.languageeng
dc.publisherUniversidade Federal de Minas Gerais
dc.rightsAcesso Aberto
dc.subjectMedicamentos
dc.subjectDoenças negligenciadas
dc.subjectDoença de Chagas
dc.subject.otherSistemas de liberação de medicamentos
dc.subject.otherNanomedicina
dc.subject.otherNanopartículas lipídicas
dc.subject.otherMedicamentos pouco solúveis em água
dc.subject.otherAnálise térmica
dc.titleEncapsulation of benznidazole in nanostructured lipid carriers and increased trypanocidal activity in a resistant Trypanosoma cruzi strain
dc.typeArtigo de periódico
local.citation.epage17
local.citation.spage1
local.citation.volume59
local.description.resumoChagas disease is a neglected parasitic disease caused by Trypanosoma cruzi, whose treatment has remained unsatisfactory for over 50 years, given that it is limited to two drugs. Benznidazole (BZN) is an efficient antichagasic drug used as the first choice, although its poor water-solubility, irregular oral absorption, low efficacy in the chronic phase, and various associated adverse effects are limiting factors for treatment. Incorporating drugs with such characteristics into nanostructured lipid carriers (NLC) is a promising alternative to overcome these limiting obstacles, enhancing drug efficacy and bioavailability while reducing toxicity. Therefore, this study proposed NLC-BZN formulations in different compositions prepared by hot-melt homogenization followed by ultrasound, and the optimized formulation was characterized by FTIR, DRX, DSC, and thermogravimetry. Biological activities included in vitro membrane toxicity (red blood cells), fibroblast cell cytotoxicity, and trypanocidal activity against epimastigotes of the Colombian strain of T. cruzi. The optimized NLC-BZN had a small size (110 nm), negative zeta potential (-18.0 mV), and high encapsulation (1.64% of drug loading), as shown by infrared spectroscopy, X-ray diffraction, and thermal analysis. The NLC-BZN also promoted lower in vitro membrane toxicity (<3% hemolysis), and 50% cytotoxic concentration (CC50) for NLC-BZN in L929 fibroblast cells (110.7 µg/mL) was twice the value as the free BZN (51.3 µg/mL). Our findings showed that the NLC-BZN had higher trypanocidal activity than free BZN against the epimastigotes of the resistant Colombian strain, and this novel NLC-BZN formulation proved to be a promising tool in treating Chagas disease and considered suitable for oral and parenteral administration.
local.publisher.countryBrasil
local.publisher.departmentFAR - DEPARTAMENTO DE ALIMENTOS
local.publisher.departmentICX - DEPARTAMENTO DE QUÍMICA
local.publisher.initialsUFMG
local.url.externahttps://www.scielo.br/j/bjps/a/RDSKVzwQv8dXXNBdmpwjN4v/?lang=en

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