In vitro schistosomicidal activity of the lignan (−)-6,6′-dinitrohinokinin (DNHK) loaded into poly(lactic-co-glycolic acid) nanoparticles against Schistosoma mansoni
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 metho...
| Main Authors: | , , , , , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2017-01-01
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| Series: | Pharmaceutical Biology |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/13880209.2017.1405996 |
| _version_ | 1818240969649160192 |
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| author | Thaís C. Lima Rodrigo Lucarini Priscilla P. Luz Emerson H. de Faria Liziane Marçal Lizandra G. Magalhães Fernanda R. Badoco Viviane R. Esperandim Eduardo F. Molina Rosangela S. Laurentz Regiane G. Lima Wilson R. Cunha Jairo K. Bastos Marcio L. Andrade Silva |
| author_facet | Thaís C. Lima Rodrigo Lucarini Priscilla P. Luz Emerson H. de Faria Liziane Marçal Lizandra G. Magalhães Fernanda R. Badoco Viviane R. Esperandim Eduardo F. Molina Rosangela S. Laurentz Regiane G. Lima Wilson R. Cunha Jairo K. Bastos Marcio L. Andrade Silva |
| author_sort | Thaís C. Lima |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-12-12T13:21:53Z |
| format | Article |
| id | doaj.art-5eea9929975044cb9f3f6107d6dc65c9 |
| institution | Directory Open Access Journal |
| issn | 1388-0209 1744-5116 |
| language | English |
| last_indexed | 2024-12-12T13:21:53Z |
| publishDate | 2017-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Pharmaceutical Biology |
| spelling | doaj.art-5eea9929975044cb9f3f6107d6dc65c92022-12-22T00:23:16ZengTaylor & Francis GroupPharmaceutical Biology1388-02091744-51162017-01-015512270227610.1080/13880209.2017.14059961405996In vitro schistosomicidal activity of the lignan (−)-6,6′-dinitrohinokinin (DNHK) loaded into poly(lactic-co-glycolic acid) nanoparticles against Schistosoma mansoniThaís C. Lima0Rodrigo Lucarini1Priscilla P. Luz2Emerson H. de Faria3Liziane Marçal4Lizandra G. Magalhães5Fernanda R. Badoco6Viviane R. Esperandim7Eduardo F. Molina8Rosangela S. Laurentz9Regiane G. Lima10Wilson R. Cunha11Jairo K. Bastos12Marcio L. Andrade Silva13Universidade de FrancaUniversidade de FrancaUniversidade Federal do Espírito Santo (UFES)Universidade de FrancaUniversidade de FrancaUniversidade de FrancaUniversidade de FrancaUniversidade de FrancaUniversidade de FrancaUniversidade Estadual PaulistaUniversidade Estadual PaulistaUniversidade de FrancaUniversity of São PauloUniversidade de FrancaContext: (−)-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.http://dx.doi.org/10.1080/13880209.2017.1405996plgabiological activitynanoparticulate formulation6,6′-dinitrohinokininschistosomicidal |
| spellingShingle | Thaís C. Lima Rodrigo Lucarini Priscilla P. Luz Emerson H. de Faria Liziane Marçal Lizandra G. Magalhães Fernanda R. Badoco Viviane R. Esperandim Eduardo F. Molina Rosangela S. Laurentz Regiane G. Lima Wilson R. Cunha Jairo K. Bastos Marcio L. Andrade Silva In vitro schistosomicidal activity of the lignan (−)-6,6′-dinitrohinokinin (DNHK) loaded into poly(lactic-co-glycolic acid) nanoparticles against Schistosoma mansoni Pharmaceutical Biology plga biological activity nanoparticulate formulation 6,6′-dinitrohinokinin schistosomicidal |
| title | In vitro schistosomicidal activity of the lignan (−)-6,6′-dinitrohinokinin (DNHK) loaded into poly(lactic-co-glycolic acid) nanoparticles against Schistosoma mansoni |
| title_full | In vitro schistosomicidal activity of the lignan (−)-6,6′-dinitrohinokinin (DNHK) loaded into poly(lactic-co-glycolic acid) nanoparticles against Schistosoma mansoni |
| title_fullStr | In vitro schistosomicidal activity of the lignan (−)-6,6′-dinitrohinokinin (DNHK) loaded into poly(lactic-co-glycolic acid) nanoparticles against Schistosoma mansoni |
| title_full_unstemmed | In vitro schistosomicidal activity of the lignan (−)-6,6′-dinitrohinokinin (DNHK) loaded into poly(lactic-co-glycolic acid) nanoparticles against Schistosoma mansoni |
| title_short | In vitro schistosomicidal activity of the lignan (−)-6,6′-dinitrohinokinin (DNHK) loaded into poly(lactic-co-glycolic acid) nanoparticles against Schistosoma mansoni |
| title_sort | in vitro schistosomicidal activity of the lignan 6 6 dinitrohinokinin dnhk loaded into poly lactic co glycolic acid nanoparticles against schistosoma mansoni |
| topic | plga biological activity nanoparticulate formulation 6,6′-dinitrohinokinin schistosomicidal |
| url | http://dx.doi.org/10.1080/13880209.2017.1405996 |
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