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

RUIZ MA; BRUNO-BLANCH LE; SCIOLI MONTOTO S; DI IANNI M; CASTRO GR; ISLAN GA; TALEVI A

Conferencia; Internation Conference on Current Trends in Biotechnology; 2016

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