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Food Chem Toxicol ; 85: 2-9, 2015 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-26260749

RESUMEN

Lupeol exhibits anti-inflammatory effects; unfortunately it shows low water solubility. An alternative to overcome this is the development of nanomaterials. Several methods for nanomaterial production are available. One of them is emulsification/solvent-evaporation. The objective of the present work was to evaluate physical properties, transport and in vitro modulator effects on NF-κB of poly (lactide-co-glycolide) (PLGA) nanoparticles loaded with lupeol. Nanonutraceuticals were prepared with 16% (w/v) of lupeol. Size distribution and morphology were measured by particle size analyzer and TEM. In vitro release of lupeol was studied by three different models: Higuchi, Siepmann & Peppas, and Power law. Transport of nanonutraceutical was studied in a Caco-2 cell model and by GC-MS. Modulator effect on NK-κB was studied by western blot analysis. Nanonutraceuticals were 10% larger than the nanoparticles without lupeol (372 vs 337 nm) and presented a broader size distribution (0.28 vs 0.22). TEM results displayed spherical structures with a broader size distribution. Entrapment efficiency of lupeol was 64.54% and it in vitro release data fitted well to the Power law and Higuchi equation (R > 0.84-0.84). Strong regulation of NF-κB of nanonutraceutical was observed. It was not observed any transport across the Caco-2 cell model at the different experimental conditions.


Asunto(s)
Antiinflamatorios no Esteroideos/metabolismo , Enterocitos/metabolismo , Absorción Intestinal , FN-kappa B/metabolismo , Nanopartículas/efectos adversos , Triterpenos Pentacíclicos/metabolismo , Poliglactina 910/efectos adversos , Transporte Activo de Núcleo Celular , Algoritmos , Antiinflamatorios no Esteroideos/administración & dosificación , Antiinflamatorios no Esteroideos/análisis , Antiinflamatorios no Esteroideos/química , Células CACO-2 , Permeabilidad de la Membrana Celular , Supervivencia Celular , Fenómenos Químicos , Suplementos Dietéticos/análisis , Emulsiones , Humanos , Microscopía Electrónica de Transmisión , FN-kappa B/agonistas , FN-kappa B/antagonistas & inhibidores , Nanopartículas/química , Nanopartículas/ultraestructura , Tamaño de la Partícula , Triterpenos Pentacíclicos/administración & dosificación , Triterpenos Pentacíclicos/análisis , Triterpenos Pentacíclicos/química , Poliglactina 910/química , Polivinilos/química , Solubilidad , Tensoactivos/química
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