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

Author(s):Show less -

Lima, Thais C. ^[1] ; Magalhaes, Lizandra G. ^[1] ; Paula, Lucas A. de L. ^[1] ; Cunha, Wilson R. ^[1] ; Januario, Ana H. ^[1] ; Pauletti, Patricia M. ^[1] ; Bastos, Jairo K. ^[2] ; dos Santos, Fransergio F. ^[1] ; Forim, Moacir R. ^[3] ; Laurentiz, Rosangela S. ^[4] ; Santos, Fernanda A. ^[4] ; Orenha, Renato P. ^[1] ; Parreira, Renato L. T. ^[1] ; Fuzo, Carlos A. ^[2] ; Molina, Eduardo F. ^[1] ; Santos, Mario F. C. ^[1] ; e Silva, Marcio L. A. ^[1]

Affiliation

^[1] Univ Franca, Franca, SP - Brazil

^[2] Sch Pharmaceut Sci Ribeirao Preto USP, Ribeirao Preto, SP - Brazil

^[3] Inst Quim Sao Carlos, Sao Carlos, SP - Brazil

^[4] Univ Estadual Paulista, Fac Engn Ilha Solteira, Dept Fis & Quim, Ilha Solteira, SP - Brazil

• Document type: Journal article
• Source: NATURAL PRODUCT RESEARCH; DEC 2021.
• Web of Science Citations: 0

Abstract

Lignan dinitrohinokinin displays important biological activities, which led to the preparation of its poly-epsilon-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. (AU)

• FAPESP's process: 09/15207-4 - Evaluation of the effect of lignans and neolignans on Schistosoma mansoni: a proteomic study
• Grantee: Lizandra Guidi Magalhães
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• FAPESP's process: 10/17378-8 - Study of the immunomodulatory activity of lignans and neolignans obtained by partial synthesis and oxidative coupling as a potential in developing new antiparasitic drugs
• Grantee: Márcio Luís Andrade e Silva
• Support Opportunities: Regular Research Grants
• FAPESP's process: 18/25010-2 - Isolation and identification of green and brown propolis constituents.
• Grantee: Mário Ferreira Conceição Santos
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• FAPESP's process: 11/07623-8 - The use of quantum-mechanical methods to study the bonds and chemical interactions in self-organizing systems with applications in catalysis, medicinal chemistry, electrochromism, energy storage and conversion
• Grantee: Renato Luis Tame Parreira
• Support Opportunities: Research Grants - Young Investigators Grants
• FAPESP's process: 11/05952-4 - Preparation and characterization of polymeric nanoparticles containing (-)-6,6'-dinitrohinokinin and (±)-licarina-A as potential drugs in the assessment of the schistosomicidal activity
• Grantee: Thaís Coelho Lima
• Support Opportunities: Scholarships in Brazil - Doctorate