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Molecules. 2017 Feb 13;22(2). pii: E277. doi: 10.3390/molecules22020277.

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

Author information

1
LEPABE, Department of Chemical Engineering, Faculty of Engineering of the University of Porto, Porto 4500-465, Portugal. joana.loureiro@fe.up.pt.
2
LEPABE, Department of Chemical Engineering, Faculty of Engineering of the University of Porto, Porto 4500-465, Portugal. up201306970@fe.up.pt.
3
LEPABE, Department of Chemical Engineering, Faculty of Engineering of the University of Porto, Porto 4500-465, Portugal. bio12101@fe.up.pt.
4
UCIBIO, REQUIMTE, Department of Chemical Sciences, Faculty of Pharmacy of the University of Porto, Porto 4050-313, Portugal. rutepneves@gmail.com.
5
UCIBIO, REQUIMTE, Department of Chemical Sciences, Faculty of Pharmacy of the University of Porto, Porto 4050-313, Portugal. fontes_joana@hotmail.com.
6
UCIBIO, REQUIMTE, Department of Chemical Sciences, Faculty of Pharmacy of the University of Porto, Porto 4050-313, Portugal. cdnunes@ff.up.pt.
7
Laboratoire de la barrière hémato-encéphalique (LBHE), University Artois, EA 2465, Lens F-62300, France. emmanuel.sevin@univ-artois.fr.
8
Laboratoire de la barrière hémato-encéphalique (LBHE), University Artois, EA 2465, Lens F-62300, France. laurence.tilloy@univ-artois.fr.
9
Laboratoire de la barrière hémato-encéphalique (LBHE), University Artois, EA 2465, Lens F-62300, France. fabien.gosselet@univ-artois.fr.
10
LEPABE, Department of Chemical Engineering, Faculty of Engineering of the University of Porto, Porto 4500-465, Portugal. mcoelho@fe.up.pt.
11
LEPABE, Department of Chemical Engineering, Faculty of Engineering of the University of Porto, Porto 4500-465, Portugal. mcsp@fe.up.pt.

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.

KEYWORDS:

Alzheimer’s disease; antibodies; blood-brain barrier; drug delivery systems; grape extracts; immuno SLN; resveratrol

PMID:
28208831
DOI:
10.3390/molecules22020277
[Indexed for MEDLINE]
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