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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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Project description:Glioblastoma (GBM) therapy is highly challenging, as the tumors are very aggressive due to infiltration into the surrounding normal brain tissue. Even a combination of the available therapeutic regimens may not debulk the tumor completely. GBM tumors are also known for recurrence, resulting in survival rates averaging <18 months. In addition, systemic chemotherapy for GBM has been challenged for its minimal desired therapeutic effects and unwanted side effects.We hypothesized that paclitaxel (PTX) and superparamagnetic iron oxide (SPIO)-loaded PEGylated poly(lactic-co-glycolic acid) (PLGA)-based nanoparticles (NPs; PTX/SPIO-NPs) can serve as an effective nanocarrier system for magnetic targeting purposes, and we aimed to demonstrate the therapeutic efficacy of this system in an orthotopic murine GBM model.PTX/SPIO-NPs were prepared by emulsion-diffusion-evaporation method and characterized for physicochemical properties. In vitro cellular uptake of PTX/SPIO-NPs was evaluated by fluorescence microscopy and Prussian blue staining. Orthotopic U87MG tumor model was used to evaluate blood-brain barrier disruption using T1 contrast agent, ex vivo biodistribution, in vivo toxicity and in vivo antitumor efficacy of PTX/SPIO-NPs.PTX/SPIO-NPs were in the size of 250 nm with negative zeta potential. Qualitative cellular uptake studies showed that the internalization of NPs was concentration dependent. Through magnetic resonance imaging, we observed that the blood-brain barrier was disrupted in the GBM area. An ex vivo biodistribution study showed enhanced accumulation of NPs in the brain of GBM-bearing mice with magnetic targeting. Short-term in vivo safety evaluation showed that the NPs did not induce any systemic toxicity compared with Taxol® (PTX). When tested for in vivo efficacy, the magnetic targeting treatment significantly prolonged the median survival time compared with the passive targeting and control treatments.Overall, PTX/SPIO-NPs with magnetic targeting could be considered as an effective anticancer targeting strategy for GBM chemotherapy.

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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