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In vitro schistosomicidal activity of the lignan (-)-6,6'-dinitrohinokinin (DNHK) loaded into poly(lactic-co-glycolic acid) nanoparticles against Schistosoma mansoni.

ABSTRACT: CONTEXT(-)-6,6'-Dinitrohinokinin (DNHK) display remarkable antiparasitic activity and was, therefore, incorporated into a nanoparticle formulation.OBJECTIVEIncorporation of DNHK in poly lactic-co-glycolic acid (PLGA) nanoparticles aiming to improve its biological activities.MATERIALS AND METHODSSynthesis, 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?µM 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.RESULTSThe 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?µM of DNHK-loaded PLGA. The groups incubated with 150 and 200?µM of DNHK-loaded PLGA for 24 and 120?h killed 100% of adult worms, afforded LC50 values of 137.0?±?2.12?µM and 79.01?±?1.90?µM, respectively, which was similar to the effect displayed by 10?µM of praziquantel.DISCUSSION AND CONCLUSIONSThe 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.

SUBMITTER: Lima TC

PROVIDER: S-EPMC6130564 | biostudies-literature | 2017 Dec

REPOSITORIES: biostudies-literature

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In vitro schistosomicidal activity of the lignan (-)-6,6'-dinitrohinokinin (DNHK) loaded into poly(lactic-co-glycolic acid) nanoparticles against Schistosoma mansoni.

Lima Thaís C TC Lucarini Rodrigo R Luz Priscilla P PP de Faria Emerson H EH Marçal Liziane L Magalhães Lizandra G LG Badoco Fernanda R FR Esperandim Viviane R VR Molina Eduardo F EF Laurentz Rosangela S RS Lima Regiane G RG Cunha Wilson R WR Bastos Jairo K JK Silva Marcio L Andrade MLA

Pharmaceutical biology 20171201 1

<h4>Context</h4>(-)-6,6'-Dinitrohinokinin (DNHK) display remarkable antiparasitic activity and was, therefore, incorporated into a nanoparticle formulation.<h4>Objective</h4>Incorporation of DNHK in poly lactic-co-glycolic acid (PLGA) nanoparticles aiming to improve its biological activities.<h4>Materials and methods</h4>Synthesis, characterization and incorporation of DNHK into glycolic acid (PLGA) nanoparticles by nanoprecipitation method. The nanoparticles were characterized by ultraviolet-vi ...[more]

PMID: 29172838

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Dataset Information

In vitro schistosomicidal activity of the lignan (-)-6,6'-dinitrohinokinin (DNHK) loaded into poly(lactic-co-glycolic acid) nanoparticles against Schistosoma mansoni.

Publications

In vitro schistosomicidal activity of the lignan (-)-6,6'-dinitrohinokinin (DNHK) loaded into poly(lactic-co-glycolic acid) nanoparticles against Schistosoma mansoni.

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