Quercetin lipid nanoparticles functionalized with transferrin for Alzheimer's disease.
Alzheimer Disease
/ drug therapy
Amyloid beta-Peptides
Blood-Brain Barrier
/ metabolism
Brain
/ metabolism
Cell Line
Cell Survival
Drug Carriers
/ chemistry
Drug Delivery Systems
/ methods
Endothelial Cells
/ metabolism
Humans
Lipids
/ chemistry
Nanoparticles
/ chemistry
Particle Size
Quercetin
/ administration & dosage
Transferrin
/ chemistry
Amyloid-beta peptide
Blood-brain barrier
Nanostructured lipid carriers (NLC)
Solid lipid nanoparticles (SLN)
Transferrin receptors
Journal
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
ISSN: 1879-0720
Titre abrégé: Eur J Pharm Sci
Pays: Netherlands
ID NLM: 9317982
Informations de publication
Date de publication:
30 May 2020
30 May 2020
Historique:
received:
16
10
2019
revised:
16
03
2020
accepted:
17
03
2020
pubmed:
23
3
2020
medline:
5
1
2021
entrez:
23
3
2020
Statut:
ppublish
Résumé
Quercetin was encapsulated in lipid nanoparticles (SLN and NLC) to take advantage of its neuroprotective properties in Alzheimer's disease. The nanoparticles were functionalized with transferrin to facilitate the passage across the blood-brain barrier through the transferrin receptors overexpressed in brain endothelial cells. NMR and FTIR confirmed the functionalization of the nanoparticles with transferrin. TEM results showed all nanoparticles presented spherical morphology. Nanoparticles exhibited size around 200 nm and zeta potential values higher than -30 mV. Quercetin entrapment efficiency was around 80-90%. LDH cytotoxicity assays in hCMEC/D3 cell line demonstrated that even for the highest concentration (30 μM) nanoparticles did not reveal cytotoxicity after 4 h of incubation. Permeability studies across hCMEC/D3 cell monolayers showed NLC permeate more the blood-brain barrier, while amyloid-beta studies demonstrated NLC-transferrin have the capacity to inhibit fibril formation. Nanoparticles seem to be suitable for brain applications, mainly for Alzheimer's disease due to inhibition of amyloid-beta aggregation.
Identifiants
pubmed: 32200044
pii: S0928-0987(20)30103-2
doi: 10.1016/j.ejps.2020.105314
pii:
doi:
Substances chimiques
Amyloid beta-Peptides
0
Drug Carriers
0
Lipids
0
Transferrin
0
Quercetin
9IKM0I5T1E
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
105314Informations de copyright
Copyright © 2020 Elsevier B.V. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of Competing Interest None