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RVG29-Functionalized Lipid Nanoparticles for Quercetin Brain Delivery and Alzheimer's Disease
R G R Pinheiro1, A Granja1, J A Loureiro2
1LAQV, REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, 4050-313, Porto, Portugal.
RVG29-functionalized nanoparticles efficiently deliver quercetin to the brain, crossing the blood-brain barrier and inhibiting amyloid-beta aggregation for Alzheimer's disease treatment.
Area of Science:
- Nanotechnology
- Neuroscience
- Pharmacology
Background:
- Alzheimer's disease is characterized by amyloid-beta aggregation.
- Effective drug delivery to the brain is a major challenge.
- Quercetin possesses neuroprotective properties.
Purpose of the Study:
- To develop RVG29-functionalized lipid nanoparticles (SLN and NLC) for targeted brain delivery.
- To load nanoparticles with quercetin for neuroprotection.
- To investigate their potential in Alzheimer's disease therapy.
Main Methods:
- Nanoparticle characterization using NMR, FTIR, TEM, and DLS.
- In vitro studies using hCMEC/D3 cell line (blood-brain barrier model).
- Amyloid-beta fibrillation inhibition assay (Thioflavin T).
Main Results:
- RVG29-nanoparticles showed suitable size (<250 nm) and zeta potential (-20 to -25 mV).
- High quercetin entrapment efficiency (>80%, NLC up to 90%).
- Enhanced blood-brain barrier permeability (1.5-fold) and inhibited amyloid-beta aggregation.
Conclusions:
- RVG29-nanoparticles efficiently deliver quercetin across the blood-brain barrier.
- This nanosystem demonstrates potential for Alzheimer's disease treatment by targeting the BBB and protecting neurons.
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