In vitro schistosomicidal activity of the lignan ( )-6,60-dinitrohinokinin (dnhk) loaded into poly(lactic-co-glycolic acid) nanoparticles against schistosoma mansoni
dc.contributor.author | Lima, Thaís C. | |
dc.contributor.author | Lucarini, Rodrigo | |
dc.contributor.author | Luz, Priscilla P. | |
dc.contributor.author | de Faria, Emerson H. | |
dc.contributor.author | Marçal, Liziane | |
dc.contributor.author | Magalhães, Lizandra G. | |
dc.contributor.author | Badoco, Fernanda R. | |
dc.contributor.author | Esperandim, Viviane R. | |
dc.contributor.author | Molina, Eduardo F. | |
dc.contributor.author | Laurentz, Rosangela S. [UNESP] | |
dc.contributor.author | Lima, Regiane G. [UNESP] | |
dc.contributor.author | Cunha, Wilson R. | |
dc.contributor.author | Bastos, Jairo K. | |
dc.contributor.author | Andrade Silva, Marcio L. | |
dc.contributor.institution | Universidade de Franca | |
dc.contributor.institution | Universidade Federal do Espírito Santo (UFES) | |
dc.contributor.institution | Universidade Estadual Paulista (UNESP) | |
dc.contributor.institution | Universidade de São Paulo (USP) | |
dc.date.accessioned | 2022-04-28T19:09:41Z | |
dc.date.available | 2022-04-28T19:09:41Z | |
dc.date.issued | 2017-01-01 | |
dc.description.abstract | Context: ( )-6,60-Dinitrohinokinin (DNHK) display remarkable antiparasitic activity and was, therefore, incorporated into a nanoparticle formulation. Objective: Incorporation of DNHK in poly lactic-co-glycolic acid (PLGA) nanoparticles aiming to improve its biological activities. Materials and methods: Synthesis, characterization and incorporation of DNHK into glycolic acid (PLGA) nanoparticles by nanoprecipitation method. The nanoparticles were characterized by ultraviolet-visible spectroscopy, X-ray diffraction, field emission electron microscopic scanning mansoni (FESEM), and dynamic light scattering (DLS). For the in vitro test with Schistosoma mansoni, the DNHK-loaded PLGA was diluted into the medium, and added at concentrations 10–200 mM to the culture medium containing one adult worm pair. The parasites were kept for 120 h and monitored every 24 h to evaluate their general condition, including: pairing, alterations in motor activity and mortality. Results: The loaded PLGA nanoparticles gave an encapsulation efficiency of 42.2% and showed spherical characteristics in monodisperse polymeric matrix. The adult worm pairs were separated after 120 h of incubation for concentrations higher than 50 mM of DNHK-loaded PLGA. The groups incubated with 150 and 200 mM of DNHK-loaded PLGA for 24 and 120 h killed 100% of adult worms, afforded LC50 values of 137.0 ± 2.12 mM and 79.01 ± 1.90 mM, respectively, which was similar to the effect displayed by 10 mM of praziquantel. Discussion and conclusions: The incorporation of DNHK-loaded showed schistosomicidal activity and allowed its sustained release. The loaded PLGA system can be administered intravenously, as well as it may be internalized by endocytosis by the target organisms. | en |
dc.description.affiliation | Laboratório de Pesquisa em Microbiologia Aplicada Núcleo de Ciências Exatas e Tecnológicas Universidade de Franca | |
dc.description.affiliation | Departamento de Química–CCE Universidade Federal do Espírito Santo (UFES) | |
dc.description.affiliation | Faculdade de Engenharia de Ilha Solteira Universidade Estadual Paulista | |
dc.description.affiliation | School of Pharmaceutical Sciences of Ribeirão Preto University of São Paulo | |
dc.description.affiliationUnesp | Faculdade de Engenharia de Ilha Solteira Universidade Estadual Paulista | |
dc.format.extent | 2270-2276 | |
dc.identifier | http://dx.doi.org/10.1080/13880209.2017.1405996 | |
dc.identifier.citation | Pharmaceutical Biology, v. 55, n. 1, p. 2270-2276, 2017. | |
dc.identifier.doi | 10.1080/13880209.2017.1405996 | |
dc.identifier.issn | 1744-5116 | |
dc.identifier.issn | 1388-0209 | |
dc.identifier.scopus | 2-s2.0-85049865641 | |
dc.identifier.uri | http://hdl.handle.net/11449/221116 | |
dc.language.iso | eng | |
dc.relation.ispartof | Pharmaceutical Biology | |
dc.source | Scopus | |
dc.subject | 6, 60-dinitrohinokinin | |
dc.subject | Biological activity | |
dc.subject | Nanoparticulate formulation | |
dc.subject | PLGA | |
dc.subject | Schistosomicidal | |
dc.title | In vitro schistosomicidal activity of the lignan ( )-6,60-dinitrohinokinin (dnhk) loaded into poly(lactic-co-glycolic acid) nanoparticles against schistosoma mansoni | en |
dc.type | Artigo |