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Title: Increased body exposure to new anti-trypanosomal through nanoencapsulation.
Authors: Branquinho, Renata Tupinambá
Lana, Gwenaelle Elza Nathalie Pound
Milagre, Matheus Marques
Guimarães, Dênia Antunes Saúde
Vilela, José Mário Carneiro
Andrade, Margareth Spangler
Lana, Marta de
Mosqueira, Vanessa Carla Furtado
Issue Date: 2017
Citation: BRANQUINHO, R. T. et al. Increased body exposure to new anti-trypanosomal through nanoencapsulation. Scientific Reports, v. 7, p. 1-12, 2017. Disponível em: <>. Acesso em: 25 fev. 2019.
Abstract: Lychnopholide, a lipophilic sesquiterpene lactone, is efficacious in mice at the acute and chronic phases of Chagas disease. Conventional poly-ε-caprolactone (PCL) and long-circulating poly(D,L-lactide)-block-polyethylene glycol (PLA-PEG) nanocapsules containing lychnopholide were developed and characterized. Lychnopholide presented high association efficiency (>90%) with the nanocapsules. A new, fast and simple HPLC-UV-based bioanalytical method was developed, validated in mouse plasma and applied to lychnopholide quantification in in vitro release kinetics and pharmacokinetics. The nanocapsules had mean hydrodynamic diameters in the range of 100–250 nm, negative zeta potentials (−30 mV to −57 mV), with good physical stability under storage. Atomic force microscopy morphological analysis revealed spherical monodispersed particles and the absence of lychnopholide crystallization or aggregation. Association of lychnopholide to PLA-PEG nanocapsules resulted in a 16-fold increase in body exposure, a 26-fold increase in plasma half-life and a dramatic reduction of the lychnopholide plasma clearance (17-fold) in comparison with free lychnopholide. The improved pharmacokinetic profile of lychnopholide in long-circulating nanocapsules is in agreement with the previously reported improved efficacy observed in Trypanosoma cruzi-infected mice. The present lychnopholide intravenous dosage form showed great potential for further pre-clinical and clinical studies in Chagas disease and cancer therapies.
ISSN: 20452322
metadata.dc.rights.license: This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. Fonte: o próprio artigo
Appears in Collections:DEFAR - Artigos publicados em periódicos

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