Artículo
Carbamazepine-loaded solid lipid nanoparticles and nanostructured lipid carriers: Physicochemical characterization and in vitro/in vivo evaluation
Scioli Montoto, Sebastián
; Sbaraglini, Maria Laura
; Talevi, Alan
; Couyoupetrou, Luis Mario; Di Ianni, Mauricio Emiliano
; Pesce, Guido Oscar; Alvarez, Vera Alejandra
; Bruno Blanch, Luis Enrique; Castro, Guillermo Raul
; Ruiz, María Esperanza
; Islan, German Abel
Fecha de publicación:
07/2018
Editorial:
Elsevier Science
Revista:
Colloids and Surfaces B: Biointerfaces
ISSN:
0927-7765
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) represent promising alternatives for drug delivery to the central nervous system. In the present work, four different nanoformulations of the antiepileptic drug Carbamazepine (CBZ) were designed and prepared by the homogenization/ultrasonication method, with encapsulation efficiencies ranging from 82.8 to 93.8%. The formulations remained stable at 4 °C for at least 3 months. Physicochemical and microscopic characterization were performed by photon correlation spectroscopy (PCS), transmission electron microscopy (TEM), atomic force microscopy (AFM); thermal properties by differential scanning calorimetry (DSC), thermogravimetry (TGA) and X-ray diffraction analysis (XRD). The results indicated the presence of spherical shape nanoparticles with a mean particle diameter around 160 nm in a narrow size distribution; the entrapped CBZ displayed an amorphous state. The in vitro release profile of CBZ fitted into a Baker-Lonsdale model for spherical matrices and almost the 100% of the encapsulated drug was released in a controlled manner during the first 24 h. The apparent permeability of CBZ-loaded nanoparticles through a cell monolayer model was similar to that of the free drug. In vivo experiments in a mice model of seizure suggested protection by CBZ-NLC against seizures for at least 2 h after intraperitoneal administration. The developed CBZ-loaded lipid nanocarriers displayed optimal characteristics of size, shape and drug release and possibly represent a promising tool to improve the treatment of refractory epilepsy linked to efflux transporters upregulation.
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Articulos(CCT - LA PLATA)
Articulos de CTRO.CIENTIFICO TECNOL.CONICET - LA PLATA
Articulos de CTRO.CIENTIFICO TECNOL.CONICET - LA PLATA
Articulos(CINDEFI)
Articulos de CENT.DE INV EN FERMENTACIONES INDUSTRIALES (I)
Articulos de CENT.DE INV EN FERMENTACIONES INDUSTRIALES (I)
Articulos(INTEMA)
Articulos de INST.DE INV.EN CIENCIA Y TECNOL.MATERIALES (I)
Articulos de INST.DE INV.EN CIENCIA Y TECNOL.MATERIALES (I)
Citación
Scioli Montoto, Sebastián; Sbaraglini, Maria Laura; Talevi, Alan; Couyoupetrou, Luis Mario; Di Ianni, Mauricio Emiliano; et al.; Carbamazepine-loaded solid lipid nanoparticles and nanostructured lipid carriers: Physicochemical characterization and in vitro/in vivo evaluation; Elsevier Science; Colloids and Surfaces B: Biointerfaces; 167; 7-2018; 73-81
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