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

• Autor(a) principal: Lima, Thais C.
• Data de Publicação: 2021
• Outros Autores: 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. [UNESP], Santos, Fernanda A. [UNESP], Orenha, Renato P., Parreira, Renato L. T., Fuzo, Carlos A., Molina, Eduardo F., Santos, Mario F. C., Silva, Márcio L. A. e
• Tipo de documento: Artigo
• Idioma: eng
• Título da fonte: Repositório Institucional da UNESP
• Texto Completo: http://dx.doi.org/10.1080/14786419.2021.2021515; http://hdl.handle.net/11449/230146
• topic: (−)-6,6’-dinitrohinokinin (DNHK); anti-inflammatory activity; polymeric nanoparticles; schistosomicidal activity

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.