Physicochemical characterization of lipid nanosystems based on natural vegetable derived esters for antiepileptic drug delivery

SEBASTIÁN SCIOLI MONTOTO; GERMAN ISLAN; MARÍA ESPERANZA RUIZ; MAURICIO DI IANNI; ALAN TALEVI; LUIS BRUNO-BLANCH; GUILLERMO R. CASTRO

Vellore

Congreso; International Conference on Current Trends in Biotechnology; 2016

School of Bio Sciences and Technology, VIT University, Vellore - The Biotech Research Society, India

Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) are promising alternatives for drug delivery to the central nervous system (CNS). In the present work, four different formulations of the antiepileptic drug Carbamazepina (CBZ) were designed and prepared by the ultrasonication technique. Characterization consisted in measuring the entrapment efficiency using an HPLC method, particle size analysis by photon correlation spectroscopy (PCS), transmission electron (TEM) and atomic force microscopy (AFM), thermal properties by differential scanning calorimetry (DSC) and thermogravimetry analysis (TGA), and structural analysis by X-ray diffraction (XRD). In vitro kinetic release of CBZ behaviour was determined as well. All formulations showed high loading capacity (82.78-93.84%) and spherical shape, with a mean particle size of 163 nm. The in vitro release profile fitted into a Baker and Lonsdale model for spherical matrices achieving almost 100% of the drug released at 24 hours. Finally, DSC, TGA and XRD evidenced that CBZ was in an amorphous state or molecularly dispersed within the lipid matrix. As conclusion, we were able to develop lipid nanosystems containing CBZ with optimal characteristics of size, shape and release to be use as drug delivery systems to address refractory epilepsy linked to ABC transporters upregulation.