Physicochemical and Biopharmaceutical Characterization of Oxcarbazepine-loaded Nanoestructured Lipid Carriers as potential antiepileptic devices

SCIOLI MONTOTO, S.; MURACA GIULIANA; DI IANNI, MAURICIO E.; MANUEL COUYOUPETROU; GUIDO PESCE; ISLAN, G.A.; YAMIL CHAIN; MARÍA ELENA VELA; MARÍA E. RUIZ; ALAN TALEVI; CASTRO GUILLERMO R.

JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY

EDITIONS SANTE

Año: 2021 vol. 63

1773-2247

Epilepsy is the second most common chronic central nervous system disorder.Oxcarbazepine (OXC) is a class II antiepileptic drug used for focal as well as forgeneralized seizures. Encapsulation of OXC in nanostructured lipid carriers (NLC)composed of cetyl palmitate and oleic acid were coated with polyvinyl alcohol (PVA) orchitosan (Ch) to obtain negative and positive surface charge nanoparticles,respectively. All NLCs displayed 97-98% OXC encapsulation efficiency, 14.5-14.6%drug loading, 121.8 to 212.3 nm size range depending on the composition andpolydispersity between 0.248-0.282 nm. The homogeneity of the NLC was confirmedby electron microscopy. OXC kinetic release from the NLCs was tested with threestructured models and the best fit was with Korsmeyer-Peppas suggesting a mixedrelease mechanism driven by diffusion rearrangement of the coating polymeric chains.In vitro Permeability studies using MDCK-MDR1 cells revealed enhanced permeabilityof the encapsulated drug compared with OXC free drug. Surface plasmon resonance tested in presence of BSA, IgG or IgM revealed no interaction with naked and PVA-coated NLCs, but do not provide relevant information regarding the Ch-coated NLC.These promising results allow to consider further in vivo studies to deliver antiepilepticdrugs like OXC efficiently