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

Autor: Thais C. Lima, Lizandra G. Magalhães, Lucas A. de L. Paula, Wilson R. Cunha, Ana H. Januário, Patricia M. Pauletti, Jairo K. Bastos, Fransergio F. dos Santos, Moacir R. Forim, Rosangela S. Laurentiz, Fernanda A. Santos, Renato P. Orenha, Renato L. T. Parreira, Carlos A. Fuzo, Eduardo F. Molina, Mario F. C. Santos, Márcio L. A. e Silva
Přispěvatelé: Universidade de Franca, Universidade de São Paulo (USP), Instituto de Química de São Carlos, Universidade Estadual Paulista (UNESP)
Rok vydání: 2021
Předmět:
Zdroj: Scopus
Repositório Institucional da UNESP
Universidade Estadual Paulista (UNESP)
instacron:UNESP
ISSN: 1478-6427
1478-6419
DOI: 10.1080/14786419.2021.2021515
Popis: Made available in DSpace on 2022-04-29T08:38:08Z (GMT). No. of bitstreams: 0 Previous issue date: 2021-01-01 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. Universidade de Franca, São Paulo School of Pharmaceutical Sciences of Ribeirão Preto–USP, São Paulo Instituto de Química de São Carlos, São Paulo Departamento de Física e Química Faculdade de Engenharia de Ilha Solteira Universidade Estadual Paulista, São Paulo Departamento de Física e Química Faculdade de Engenharia de Ilha Solteira Universidade Estadual Paulista, São Paulo
Databáze: OpenAIRE
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