Characterization and trypanocidal activity of nifurtimox-containing and empty nanoparticles of polyethylcyanoacrylates

dc.contributor.authorGonzalez Martin, G
dc.contributor.authorMerino, I
dc.contributor.authorRodriguez Cabezas, MN
dc.contributor.authorTorres, M
dc.contributor.authorNunez, R
dc.contributor.authorOsuna, A
dc.date.accessioned2024-01-10T13:46:40Z
dc.date.available2024-01-10T13:46:40Z
dc.date.issued1998
dc.description.abstractThe aim of this study was to evaluate the utility of nanoparticles of polyalkylcyanoacrylate as a targeted delivery system for nifurtimox against Trypanosoma cruzi, responsible for Chagas' disease. Ethylcyanoacrylate nanoparticles were prepared by an emulsion polymerization process and formulations containing different concentrations of nifurtimox, polyethylcyanoacrylates and surfactants were investigated and analysed for size and drug content.
dc.description.abstractThe nanoparticles obtained were less than 200 nm in size, as measured by electron microscopy and cytometry. The peak percentage of nifurtimox uptake into the nanoparticles was 33.4% for use of 500 mu L polyethylcyanoacrylate, 200 mu L surfactant (Tween 20) and 10 mg nifurtimox in 50 mL polymerization medium. The highest release of nifurtimox from the nanoparticles was 65.4% after 6-h incubation at pH 7.4. In-vitro studies using cultures of T. cruzi epimastigotes revealed considerably increased trypanocidal activity compared with a standard solution of nifurtimox. Studies of cell cultures previously infected with metacyclic forms of the parasite showed that only 2-h treatment with solutions of 0.001% of the nanoparticle suspension reduced parasitism by 87-94% both when the nanoparticles were loaded with nifurtimox and when unloaded. Electron-microscopic examination revealed processes of degeneration and lysis, suggesting apoptotic processes, in intracellular amastigotes and free amastigotes treated with the nanoparticles. It was demonstrated that unloaded nanoparticles, by mechanisms not completely elucidated, have trypanocide activity similar to that of a standard solution of nifurtimox. It is concluded that the nanoparticles loaded with nifurtimox constitutes a good carrier of the drug against T. cruzi. The loaded-nanoparticles significantly increase trypanocidal activity.
dc.fechaingreso.objetodigital2024-05-14
dc.format.extent7 páginas
dc.fuente.origenWOS
dc.identifier.doi10.1111/j.2042-7158.1998.tb03301.x
dc.identifier.issn0022-3573
dc.identifier.pubmedidMEDLINE:9580223
dc.identifier.urihttps://doi.org/10.1111/j.2042-7158.1998.tb03301.x
dc.identifier.urihttps://repositorio.uc.cl/handle/11534/79186
dc.identifier.wosidWOS:000071971700004
dc.information.autorucQuímica;González G;S/I;98524
dc.issue.numero1
dc.language.isoen
dc.nota.accesocontenido parcial
dc.pagina.final35
dc.pagina.inicio29
dc.publisherROYAL PHARMACEUTICAL SOC GREAT BRITAIN
dc.revistaJOURNAL OF PHARMACY AND PHARMACOLOGY
dc.rightsacceso restringido
dc.subjectTRYPANOSOMA-CRUZI
dc.subjectDRUG-CARRIER
dc.subjectPOLYALKYLCYANOACRYLATE NANOPARTICLES
dc.subjectLIPOSOMES
dc.subjectFORMS
dc.subject.ods03 Good Health and Well-being
dc.subject.odspa03 Salud y bienestar
dc.titleCharacterization and trypanocidal activity of nifurtimox-containing and empty nanoparticles of polyethylcyanoacrylates
dc.typeartículo
dc.volumen50
sipa.codpersvinculados98524
sipa.indexWOS
sipa.indexScopus
sipa.trazabilidadCarga SIPA;09-01-2024
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