title: Lipid-based nanocarrier for quercetin delivery: system characterization and molecular interactions studies.
abstract: The flavonoid quercetin (QU) is a naturally occurring compound with several biological activities. However, the oral bioavailability of this compound is very low due to the high pre-systemic metabolism in the colon and liver and its low water solubility. In this context, the development of QU-loaded nanocarriers (NEs) is a promising approach to improve the drug oral bioavailability. This study investigates the variation of the concentration of 12-hydroxystearic acid-polyethylene glycol copolymer, lecithin and castor oil (CO) as to increase the amount of QU encapsulated while maintaining physicochemical characteristics described in previous studies. To better understand the ability to load and release the drug, we investigated the molecular interactions between QU and NE. Lipid-based NEs were prepared using CO as oily phase and PEG 660-stearate and lecithin as surfactants. Hot solvent diffusion and phase inversion temperature were methods employed to produce NEs. The QU-NEs were investigated for physicochemical characteristics and in vitro drug release. Molecular interactions between QU and the NEs were monitored through the complementary infrared (Fourier transform infrared) and NMR. The results revealed that it was possible to incorporate higher amounts of QU in a lipid-based NE with a reduced size (20 nm). The system developed allow a sustained release of QU probably due to the shell formed by the surfactants around the NE and the flavonoid ordering effect in the emulsion hydrophobic regions, which may reduce the system permeability.
authors.affiliation: a Laboratório de Nanotecnologia Aplicada à Saúde, Programa de Pós-Graduação em Ciências da Saúde , Universidade Federal do Rio Grande (FURG) , Rio Grande , RS , Brazil ;
authors.forename: Gabriela
authors.initials: G
authors.lastname: Hädrich
authors.affiliation: a Laboratório de Nanotecnologia Aplicada à Saúde, Programa de Pós-Graduação em Ciências da Saúde , Universidade Federal do Rio Grande (FURG) , Rio Grande , RS , Brazil ;
authors.forename: Samantha Oliveira
authors.initials: SO
authors.lastname: Monteiro
authors.affiliation: b Grupo de Investigação de Interações Moleculares em Membranas, Programa de Pós-Graduação em Química tecnológica e Ambiental , Universidade Federal do Rio Grande , Rio Grande , RS , Brazil ;
authors.forename: Marisa Raquel
authors.initials: MR
authors.lastname: Rodrigues
authors.affiliation: b Grupo de Investigação de Interações Moleculares em Membranas, Programa de Pós-Graduação em Química tecnológica e Ambiental , Universidade Federal do Rio Grande , Rio Grande , RS , Brazil ;
authors.forename: Vânia Rodrigues
authors.initials: VR
authors.lastname: de Lima
authors.affiliation: c Centre de Recherches sur les Macromolécules Végétales, Université Grenoble Alpes , Grenoble , France ;|d CERMAV, CNRS , Grenoble , France ;
authors.forename: Jean-Luc
authors.initials: JL
authors.lastname: Putaux
authors.affiliation: e Laboratório de Desenvolvimento Galênico, Programa de Pós-Graduação em Ciências Farmacêuticas , Universidade Federal do Rio Grande do Sul (UFRGS) , Porto Alegre , RS , Brazil.
authors.forename: Juliana
authors.initials: J
authors.lastname: Bidone
authors.affiliation: e Laboratório de Desenvolvimento Galênico, Programa de Pós-Graduação em Ciências Farmacêuticas , Universidade Federal do Rio Grande do Sul (UFRGS) , Porto Alegre , RS , Brazil.
authors.forename: Helder Ferreira
authors.initials: HF
authors.lastname: Teixeira
authors.affiliation: a Laboratório de Nanotecnologia Aplicada à Saúde, Programa de Pós-Graduação em Ciências da Saúde , Universidade Federal do Rio Grande (FURG) , Rio Grande , RS , Brazil ;
authors.forename: Ana Luiza
authors.initials: AL
authors.lastname: Muccillo-Baisch
authors.affiliation: a Laboratório de Nanotecnologia Aplicada à Saúde, Programa de Pós-Graduação em Ciências da Saúde , Universidade Federal do Rio Grande (FURG) , Rio Grande , RS , Brazil ;
authors.forename: Cristiana Lima
authors.initials: CL
authors.lastname: Dora
mesh_terms: D002368:Castor Oil / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D004347:Drug Interactions; D065546:Drug Liberation; D054709:Lecithins / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry*; D011794:Quercetin / Q000008:administration & dosage* / Q000737:chemistry; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013229:Stearic Acids / Q000737:chemistry*; D013499:Surface Properties
chemical_list: D004337:Drug Carriers; D054709:Lecithins; D013229:Stearic Acids; D011092:Polyethylene Glycols; C067028:Solutol HS 15; D002368:Castor Oil; D011794:Quercetin
keywords: Quercetin; cryo-TEM; lipid nanocarriers; molecular interactions; nanotechnology