Publication Cover
Natural Product Research
Formerly Natural Product Letters
Volume 36, 2022 - Issue 22
238
Views
1
CrossRef citations to date
0
Altmetric
Short Communications

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

, ORCID Icon, , ORCID Icon, , , , ORCID Icon, , , , , , , , & ORCID Icon show all
Pages 5872-5878 | Received 28 Jul 2021, Accepted 11 Dec 2021, Published online: 29 Dec 2021
 

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

Disclosure statement

The authors declare no conflict of interest.

Additional information

Funding

This study was funded by (FAPESP, grants # 2011/07623-8, 2011/05952-4, 2010/17378-8, 2009/15207-4 and 18/25010-2), (CAPES n°001) and (CNPq) fellowships # 313648/2018-2, 303349/2013-1, 401630/2014-5, 306271/2017-6 and 553287/2009-5.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.