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/químicaRESUMEN
Nine infants without evidence of nephropathy were studied. After a control period, furosemide, 1.0 mg/kg. of body weight, was administered intravenously and urine was collected. In all patients, urinary volume increased from a mean of 0.15 ml/min. during the control period, to 0.69 ml/min. after furosemide and urinary sodium excretion rose from 1.77 micro Eq/min. in the first period, to 50.13 micro Eq/min. in the second. There was no significant change in urinary osmolarity and in serum electrolytes. Three hours after furosemide, all children showed dehydration from light to moderate and saline infusion was necessary. No correlation was found between age and weight of the infants with the response to furosemide. Because this diuretic has an energetic action in infants as in children and adults, it must be used carefully and it is proposed that the initial dose of furosemide in infants be 0.5 mg/kg.