Morphological and release characterization of nanoparticles formulated with poly (dl-lactide-co-glycolide) (PLGA) and lupeol: In vitro permeability and modulator effect on NF-κB in Caco-2 cell system stimulated with TNF-α

• Published in: Food and chemical toxicology Vol. 85; pp. 2 - 9
• Main Authors: Cháirez-Ramírez, M.H., Sánchez-Burgos, J.A., Gomes, C., Moreno-Jiménez, M.R., González-Laredo, R.F., Bernad-Bernad, M.J., Medina-Torres, L., Ramírez-Mares, M.V., Gallegos-Infante, J.A., Rocha-Guzmán, N.E.
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01-11-2015
• Subjects: Active Transport, Cell Nucleus; Algorithms; Anti-inflammation; Anti-Inflammatory Agents, Non-Steroidal - administration & dosage; Anti-Inflammatory Agents, Non-Steroidal - analysis; Anti-Inflammatory Agents, Non-Steroidal - chemistry; Anti-Inflammatory Agents, Non-Steroidal - metabolism; Caco-2 Cells; Cell Membrane Permeability; Cell Survival; Chemical Phenomena; Dietary Supplements - analysis; Emulsions; Enterocytes - metabolism; Humans; Intestinal Absorption; Lupeol; Microscopy, Electron, Transmission; Nanoparticles; Nanoparticles - adverse effects; Nanoparticles - chemistry; Nanoparticles - ultrastructure; NF-kappa B - agonists; NF-kappa B - antagonists & inhibitors; NF-kappa B - metabolism; NF-kB; Particle Size; Pentacyclic Triterpenes - administration & dosage; Pentacyclic Triterpenes - analysis; Pentacyclic Triterpenes - chemistry; Pentacyclic Triterpenes - metabolism; Polyglactin 910 - adverse effects; Polyglactin 910 - chemistry; Polyvinyls - chemistry; Solubility; Surface-Active Agents - chemistry; Transport; Nanoparticles; Transport; Anti-inflammation; Lupeol; NF-kB
• ISSN: 0278-6915; 1873-6351
• DOI: 10.1016/j.fct.2015.08.003

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.
•In vitro release of lupeol adjust to Power law and Higuchi equation.•Strong regulation of NF-κB of nanonutraceutical was observed.•It was not observed any transport of lupeol across the Caco-2 cell model.