%0 Journal Article %A Lima, Thaís C. %A Lucarini, Rodrigo %A Luz, Priscilla P. %A H. de Faria, Emerson %A Marçal, Liziane %A Magalhães, Lizandra G. %A Badoco, Fernanda R. %A Esperandim, Viviane R. %A Molina, Eduardo F. %A Laurentz, Rosangela S. %A Lima, Regiane G. %A R. Cunha, Wilson %A Bastos, Jairo K. %A Silva, Marcio L. Andrade %D 2017 %T In vitro schistosomicidal activity of the lignan (−)-6,6′-dinitrohinokinin (DNHK) loaded into poly(lactic-co-glycolic acid) nanoparticles against Schistosoma mansoni %U https://tandf.figshare.com/articles/journal_contribution/_i_In_vitro_i_schistosomicidal_activity_of_the_lignan_-6_6_-dinitrohinokinin_DNHK_loaded_into_poly_lactic-co-glycolic_acid_nanoparticles_against_i_Schistosoma_mansoni_i_/5633740 %R 10.6084/m9.figshare.5633740 %2 https://ndownloader.figshare.com/files/9811102 %K PLGA %K biological activity %K nanoparticulate formulation %K 6,6′-dinitrohinokinin %K schistosomicidal %X

Context: (−)-6,6′-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 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.

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 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 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.

%I Taylor & Francis