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

Autor:	Lima TC; Universidade de Franca, Franca, São Paulo, Brazil., Magalhães LG; Universidade de Franca, Franca, São Paulo, Brazil., Paula LAL; Universidade de Franca, Franca, São Paulo, Brazil., Cunha WR; Universidade de Franca, Franca, São Paulo, Brazil., Januário AH; Universidade de Franca, Franca, São Paulo, Brazil., Pauletti PM; Universidade de Franca, Franca, São Paulo, Brazil., Bastos JK; School of Pharmaceutical Sciences of Ribeirão Preto - USP, Ribeirão Preto, São Paulo, Brazil., Dos Santos FF; Universidade de Franca, Franca, São Paulo, Brazil., Forim MR; Instituto de Química de São Carlos, São Carlos, São Paulo, Brazil., Laurentiz RS; Departamento de Física e Química, Faculdade de Engenharia de Ilha Solteira, Universidade Estadual Paulista, Ilha Solteira, São Paulo, Brazil., Santos FA; Departamento de Física e Química, Faculdade de Engenharia de Ilha Solteira, Universidade Estadual Paulista, Ilha Solteira, São Paulo, Brazil., Orenha RP; Universidade de Franca, Franca, São Paulo, Brazil., Parreira RLT; Universidade de Franca, Franca, São Paulo, Brazil., Fuzo CA; School of Pharmaceutical Sciences of Ribeirão Preto - USP, Ribeirão Preto, São Paulo, Brazil., Molina EF; Universidade de Franca, Franca, São Paulo, Brazil., Santos MFC; Universidade de Franca, Franca, São Paulo, Brazil., Silva MLAE; Universidade de Franca, Franca, São Paulo, Brazil.
Jazyk:	angličtina
Zdroj:	Natural product research [Nat Prod Res] 2022 Nov; Vol. 36 (22), pp. 5872-5878. Date of Electronic Publication: 2021 Dec 29.
DOI:	10.1080/14786419.2021.2021515
Abstrakt:	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.
Databáze:	MEDLINE
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