In Vitro Evaluation on a Model of Blood Brain Barrier of Idebenone-Loaded Solid Lipid Nanoparticles

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Abstract:

The aim of this study was to evaluate in vitro the permeation of the antioxidant agent Idebenone (IDE) loaded into solid lipid nanoparticles (SLN) across MDCKII-MDR1 cell monolayer, selected as an in vitro model of the Blood Brain Barrier (BBB). SLN were prepared using cetyl palmitate as solid lipid and different non-ionic surfactants, oleth-20, ceteth-20 and isoceth-20, by the phase inversion temperature (PIT) technique. The resulting SLN showed physiological pH and osmolarity values, a mean particle diameter in the range of 33–63 nm, a single peak in size distribution, and a ζ potential ranging from +3.14 to −2.89 mV. When incubating these SLN in Simulated Body Fluid (SBF), the particle size was maintained for all samples throughout the study. IDE permeability across MDCKII-MDR1 cell monolayers from the SLN under investigation was 0.40–0.53 fold lower than free IDE and no significant difference was observed comparing IDE permeation from all the SLN tested. It is noteworthy that IDE loading into SLN avoided the use of an organic solvent to solubilize IDE, a poor water soluble compound, allowing the parenteral administration of this drug in aqueous vehicles. Furthermore, the results of in vitro transport studies, performed using fluorescein-dextran 4000 (FD4) and diazepam (DZ) as markers of the paracellular pathway and the transcellular pathway, respectively, pointed out that IDE could permeate via a transcellular pathway. Therefore, these novel nanocarriers could be regarded as a promising strategy to design delivery systems for IDE administration to the brain, deserving further investigations under in vivo conditions.

Keywords: BLOOD BRAIN BARRIER; IDEBENONE; MDCKII-MDR1 CELLS; SOLID LIPID NANOPARTICLES

Document Type: Research Article

DOI: http://dx.doi.org/10.1166/jnn.2012.5174

Publication date: January 1, 2012

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  • Journal for Nanoscience and Nanotechnology (JNN) is an international and multidisciplinary peer-reviewed journal with a wide-ranging coverage, consolidating research activities in all areas of nanoscience and nanotechnology into a single and unique reference source. JNN is the first cross-disciplinary journal to publish original full research articles, rapid communications of important new scientific and technological findings, timely state-of-the-art reviews with author's photo and short biography, and current research news encompassing the fundamental and applied research in all disciplines of science, engineering and medicine.
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