Nanoemulsion composed of 10-(4,5-dihydrothiazol-2-yl)thio)decan-1-ol), a synthetic analog of 3-alkylpiridine marine alkaloid : development, characterization, and antimalarial activity.

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dc.contributor.authorSilva, Marina Goulart da
dc.contributor.authorCardoso, Jéssica Ferreira
dc.contributor.authorPerasoli, Fernanda Barçante
dc.contributor.authorBranquinho, Renata Tupinambá
dc.contributor.authorMourão, Renata Silva
dc.contributor.authorTavares, Harley da Silva
dc.contributor.authorXocaira, Maria Luiza Costa Trench
dc.contributor.authorGuimarães, Daniel Silqueira Martins
dc.contributor.authorViana, Gustavo Henrique Ribeiro
dc.contributor.authorVarotti, Fernando de Pilla
dc.contributor.authorSilva, Gisele Rodrigues da
dc.date.accessioned2021-12-06T20:23:38Z
dc.date.available2021-12-06T20:23:38Z
dc.date.issued2020pt_BR
dc.description.abstractMalaria treatment is based on a reduced number of antimalarial drugs, and drug resistance has emerged, leading to the search for new antimalarial drugs incorporated into pharmaceutical formulations. In this study, 10-(4,5- dihydrothiazol-2-yl)thio)decan-1-ol) (thiazoline), a synthetic analog of 3-alkylpiridine marine alkaloid, and a potent antimalarial substance, was incorporated into O/W nanoemulsion. This formulation was prepared by a 23 factorial design. It was characterized by globule diameter, polydispersity index, zeta potential, encapsulation efficiency, in vitro thiazoline release at pH 2 and 6.86, and accelerated stability. In vitro and in vivo antimalarial activity was determined against P. falciparum and P. berghei, respectively. Thiazoline nanoemulsion showed 248.8 nm of globule diameter, 0.236 of polydispersity index, -38.5 mV of zeta potential, 96.92% encapsulation efficiency, and it was stable for 6 months. Thiazoline release profiles differed in acidic and neutral media, but in both cases, the nanoemulsion controlled and prolonged the thiazoline delivery. Thiazoline nanoemulsion exerted in vitro antimalarial activity against the parasite (IC50 = 1.32 µM), and it significantly reduced the in vivo parasitemia for 8 days without increasing the survival time of animals. Therefore, the thiazoline nanoemulsion represents a strategy to treat malaria combining an antimalarial candidate and a new nanocarrier.pt_BR
dc.identifier.citationSILVA, M. G. da et al. Nanoemulsion composed of 10-(4,5-dihydrothiazol-2-yl)thio)decan-1-ol), a synthetic analog of 3-alkylpiridine marine alkaloid: development, characterization, and antimalarial activity. European Journal of Pharmaceutical Sciences, v. 151, p. 105382, 2020. Disponível em: <https://www.sciencedirect.com/science/article/abs/pii/S0928098720301718?via%3Dihub>. Acesso em: 10 jun. 2021.pt_BR
dc.identifier.doihttps://doi.org/10.1016/j.ejps.2020.105382 vpt_BR
dc.identifier.issn0928-0987
dc.identifier.urihttp://www.repositorio.ufop.br/jspui/handle/123456789/14099
dc.identifier.uri2https://www.sciencedirect.com/science/article/abs/pii/S0928098720301718?via%3Dihubpt_BR
dc.language.isoen_USpt_BR
dc.rightsrestritopt_BR
dc.subjectPlasmodium falciparumpt_BR
dc.subjectThiazolept_BR
dc.titleNanoemulsion composed of 10-(4,5-dihydrothiazol-2-yl)thio)decan-1-ol), a synthetic analog of 3-alkylpiridine marine alkaloid : development, characterization, and antimalarial activity.pt_BR
dc.typeArtigo publicado em periodicopt_BR
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