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Evaluation of lignan-loaded poly(ε-caprolactone) nanoparticles: synthesis, characterization, in vivo and in silico schistosomicidal activity

Lima, Thais C. ; Magalhães, Lizandra G. ; Paula, Lucas A. de L. ; Cunha, Wilson R. ; Januário, Ana H. ; Pauletti, Patricia M. ; Bastos, Jairo K. ; dos Santos, Fransergio F. ; Forim, Moacir R. ; Laurentiz, Rosangela S. ; Santos, Fernanda A. ; Orenha, Renato P. ; Parreira, Renato L. T. ; Fuzo, Carlos A. ; Molina, Eduardo F. ; Santos, Mario F. C. ; Silva, Márcio L. A. e

Natural Product Research, 2022, Vol.36 (22), p.5872-5878

Taylor & Francis

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Título:
Evaluation of lignan-loaded poly(ε-caprolactone) nanoparticles: synthesis, characterization, in vivo and in silico schistosomicidal activity
Autor: Lima, Thais C. ; Magalhães, Lizandra G. ; Paula, Lucas A. de L. ; Cunha, Wilson R. ; Januário, Ana H. ; Pauletti, Patricia M. ; Bastos, Jairo K. ; dos Santos, Fransergio F. ; Forim, Moacir R. ; Laurentiz, Rosangela S. ; Santos, Fernanda A. ; Orenha, Renato P. ; Parreira, Renato L. T. ; Fuzo, Carlos A. ; Molina, Eduardo F. ; Santos, Mario F. C. ; Silva, Márcio L. A. e
Materias: (−)-6,6'-dinitrohinokinin (DNHK) ; anti-inflammatory activity ; polymeric nanoparticles ; schistosomicidal activity
Es parte de: Natural Product Research, 2022, Vol.36 (22), p.5872-5878
Descripción: Lignan dinitrohinokinin displays important biological activities, which led to the preparation of its poly-ε-caprolactone nanoparticles. Kinetics analysis revealed initially slow drug release followed by a prolonged, moderate release 6 h later due to DNHK diffusion through the polymeric matrix. Molecular dynamics simulations show that DNHK molecules that interact stronger with other DNHK molecules near the PCL/DNHK surface are more difficult to dissociate from the nanoparticle. The smaller diameter nanocapsules with negative surface charge conferred good colloidal stability. The formulations showed a size distribution with monodisperse systems formation. In vivo evaluation of schistosomicidal activity against Schistosoma mansoni showed that DNHK, when incorporated into nanoparticles, caused egg number reduction of 4.2% and 28.1% at 40 mg/kg and 94.2% and 84.4% at 400 mg/kg in the liver and the spleen, respectively. The PCL nanoparticles were stable in aqueous dispersion and could be optimized to be used as a promising lignan release agent.
Editor: Taylor & Francis
Idioma: Inglés

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Evaluation of lignan-loaded poly(ε-caprolactone) nanoparticles: synthesis, characterization, in vivo and in silico schistosomicidal activity

Taylor & Francis

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