title: 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.
abstract: 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.
authors.affiliation: Instituto Tecnológico de Durango, Departamento de Ingenierías Química y Bioquímica, Blvd. Felipe Pescador 1830 Ote, Col Nueva Vizcaya, 34080 Durango, Dgo, Mexico.
authors.forename: M H
authors.initials: MH
authors.lastname: Cháirez-Ramírez
authors.affiliation: Instituto Tecnológico de Durango, Departamento de Ingenierías Química y Bioquímica, Blvd. Felipe Pescador 1830 Ote, Col Nueva Vizcaya, 34080 Durango, Dgo, Mexico.
authors.forename: J A
authors.initials: JA
authors.lastname: Sánchez-Burgos
authors.affiliation: Texas A&M, Dept. of Biological and Agriculture Engineering, 201 Scoates Hall I 2117 TAMU, College Station, TX 77843, USA.
authors.forename: C
authors.initials: C
authors.lastname: Gomes
authors.affiliation: Instituto Tecnológico de Durango, Departamento de Ingenierías Química y Bioquímica, Blvd. Felipe Pescador 1830 Ote, Col Nueva Vizcaya, 34080 Durango, Dgo, Mexico.
authors.forename: M R
authors.initials: MR
authors.lastname: Moreno-Jiménez
authors.affiliation: Instituto Tecnológico de Durango, Departamento de Ingenierías Química y Bioquímica, Blvd. Felipe Pescador 1830 Ote, Col Nueva Vizcaya, 34080 Durango, Dgo, Mexico.
authors.forename: R F
authors.initials: RF
authors.lastname: González-Laredo
authors.affiliation: Facultad de Química, Departamento de Ingeniería Química, Conjunto E, Universidad Nacional Autónoma de México, CU, 04510 México, DF, Mexico.
authors.forename: M J
authors.initials: MJ
authors.lastname: Bernad-Bernad
authors.affiliation: Facultad de Química, Departamento de Ingeniería Química, Conjunto E, Universidad Nacional Autónoma de México, CU, 04510 México, DF, Mexico.
authors.forename: L
authors.initials: L
authors.lastname: Medina-Torres
authors.affiliation: Instituto Tecnológico de Morelia, Departamento de Ingenierías Química y Bioquímica, Ave. Tecnológico 1500, Col. Lomas de Santiaguito, 58120 Morelia Mich, Mexico.
authors.forename: M V
authors.initials: MV
authors.lastname: Ramírez-Mares
authors.affiliation: Instituto Tecnológico de Durango, Departamento de Ingenierías Química y Bioquímica, Blvd. Felipe Pescador 1830 Ote, Col Nueva Vizcaya, 34080 Durango, Dgo, Mexico. Electronic address: agallegos@itdurango.edu.mx.
authors.forename: J A
authors.initials: JA
authors.lastname: Gallegos-Infante
authors.affiliation: Instituto Tecnológico de Durango, Departamento de Ingenierías Química y Bioquímica, Blvd. Felipe Pescador 1830 Ote, Col Nueva Vizcaya, 34080 Durango, Dgo, Mexico. Electronic address: nrocha@itdurango.edu.mx.
authors.forename: N E
authors.initials: NE
authors.lastname: Rocha-Guzmán
mesh_terms: D021581:Active Transport, Cell Nucleus; D000465:Algorithms; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000032:analysis / Q000737:chemistry / Q000378:metabolism*; D018938:Caco-2 Cells; D002463:Cell Membrane Permeability; D002470:Cell Survival; D055598:Chemical Phenomena; D019587:Dietary Supplements / Q000032:analysis; D004655:Emulsions; D020895:Enterocytes / Q000378:metabolism*; D006801:Humans; D007408:Intestinal Absorption; D046529:Microscopy, Electron, Transmission; D016328:NF-kappa B / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism*; D053758:Nanoparticles / Q000009:adverse effects* / Q000737:chemistry / Q000648:ultrastructure; D010316:Particle Size; D053978:Pentacyclic Triterpenes / Q000008:administration & dosage / Q000032:analysis / Q000737:chemistry / Q000378:metabolism*; D011098:Polyglactin 910 / Q000009:adverse effects* / Q000737:chemistry; D011145:Polyvinyls / Q000737:chemistry; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry; D000094042:Lupanes
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004655:Emulsions; D016328:NF-kappa B; D053978:Pentacyclic Triterpenes; D011098:Polyglactin 910; D011145:Polyvinyls; D013501:Surface-Active Agents; C013215:polyvinyl acetate; C010480:lupeol; D000094042:Lupanes
keywords: Anti-inflammation; Lupeol; NF-kB; Nanoparticles; Transport