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Molecules 2017, 22(2), 277; doi:10.3390/molecules22020277

Resveratrol and Grape Extract-loaded Solid Lipid Nanoparticles for the Treatment of Alzheimer’s Disease

1
LEPABE, Department of Chemical Engineering, Faculty of Engineering of the University of Porto, Porto 4500-465, Portugal
2
UCIBIO, REQUIMTE, Department of Chemical Sciences, Faculty of Pharmacy of the University of Porto, Porto 4050-313, Portugal
3
Laboratoire de la barrière hémato-encéphalique (LBHE), University Artois, EA 2465, Lens F-62300, France
*
Author to whom correspondence should be addressed.
Academic Editor: Norbert Latruffe
Received: 6 December 2016 / Revised: 26 January 2017 / Accepted: 1 February 2017 / Published: 13 February 2017
(This article belongs to the Special Issue Improvements for Resveratrol Efficacy)
View Full-Text   |   Download PDF [3863 KB, uploaded 13 February 2017]   |  

Abstract

The aggregation of amyloid-β peptide (Aβ) has been linked to the formation of neuritic plaques, which are pathological hallmarks of Alzheimer’s disease (AD). Various natural compounds have been suggested as therapeutics for AD. Among these compounds, resveratrol has aroused great interest due to its neuroprotective characteristics. Here, we provide evidence that grape skin and grape seed extracts increase the inhibition effect on Aβ aggregation. However, after intravenous injection, resveratrol is rapidly metabolized into both glucuronic acid and sulfate conjugations of the phenolic groups in the liver and intestinal epithelial cells (within less than 2 h), which are then eliminated. In the present study, we show that solid lipid nanoparticles (SLNs) functionalized with an antibody, the anti-transferrin receptor monoclonal antibody (OX26 mAb), can work as a possible carrier to transport the extract to target the brain. Experiments on human brain-like endothelial cells show that the cellular uptake of the OX26 SLNs is substantially more efficient than that of normal SLNs and SLNs functionalized with an unspecific antibody. As a consequence, the transcytosis ability of these different SLNs is higher when functionalized with OX-26. View Full-Text
Keywords: resveratrol; grape extracts; Alzheimer’s disease; immuno SLN; blood-brain barrier; antibodies; drug delivery systems resveratrol; grape extracts; Alzheimer’s disease; immuno SLN; blood-brain barrier; antibodies; drug delivery systems
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Loureiro, J.A.; Andrade, S.; Duarte, A.; Neves, A.R.; Queiroz, J.F.; Nunes, C.; Sevin, E.; Fenart, L.; Gosselet, F.; Coelho, M.A.N.; Pereira, M.C. Resveratrol and Grape Extract-loaded Solid Lipid Nanoparticles for the Treatment of Alzheimer’s Disease. Molecules 2017, 22, 277.

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