Evaluation of lignan-loaded poly(ε-caprolactone) nanoparticles: synthesis, characterization, in vivo and in silico schistosomicidal activity. Issue 22 (17th November 2022)

• Record Type: Journal Article
• Authors: 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
• Is Part Of: Natural product research. Volume 36:Issue 22(2022)
• Page Start: 5872
• Page End: 5878
• Publication Date: 2022-11-17
• Subjects: (−)-6, 6'-dinitrohinokinin (DNHK) -- polymeric nanoparticles -- schistosomicidal activity -- anti-inflammatory activity; Natural products -- Periodicals; Natural products -- Research -- Periodicals; Biological Factors -- Periodicals; Biological Products -- Periodicals; 547
• DOI: 10.1080/14786419.2021.2021515
• Languages: English
• ISSNs: 1478-6419

Abstract

Abstract: 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. Graphical Abstract: UF0001