Brain-targeted delivery of resveratrol using solid lipid nanoparticles functionalized with apolipoprotein E.

Area of Science:

• Nanotechnology
• Neuroscience
• Pharmacology

Background:

• Resveratrol exhibits neuroprotective properties.
• Solid lipid nanoparticles (SLNs) offer a promising drug delivery system.
• Apolipoprotein E (ApoE) facilitates transport across the blood-brain barrier (BBB) via LDL receptors.

Purpose of the Study:

• To develop and characterize resveratrol-loaded SLNs functionalized with ApoE for improved brain targeting.
• To evaluate the in vitro safety and efficacy of these nanocarriers for resveratrol delivery.

Main Methods:

• Synthesis and characterization of ApoE-functionalized resveratrol-loaded SLNs using Transmission Electron Microscopy and Dynamic Light Scattering.
• In vitro cytotoxicity assessment using MTT and LDH assays on hCMEC/D3 cells.
• Evaluation of enhanced BBB permeability using hCMEC/D3 cell monolayers.

Main Results:

• Characterization confirmed spherical nanoparticles with a Z-average < 200 nm, zeta potential of -13 mV, and ~90% resveratrol entrapment efficiency.
• No significant cytotoxicity was observed for the nanoparticles up to 50 μM over 4 hours.
• ApoE-functionalized SLNs demonstrated a 1.8-fold increase in resveratrol permeability across the BBB model compared to non-functionalized SLNs.

Conclusions:

• ApoE-functionalized SLNs represent a viable strategy for delivering resveratrol into the brain.
• This nanosystem protects resveratrol from degradation in circulation.
• The enhanced BBB permeability suggests potential for treating neurological disorders with resveratrol.