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Updated: Feb 10, 2026

A Technique to Functionalize and Self-assemble Macroscopic Nanoparticle-ligand Monolayer Films onto Template-free Substrates
Published on: May 9, 2014
Brain Targeting Delivery Facilitated by Ligand-Functionalized Layered Double Hydroxide Nanoparticles
Weiyu Chen, Huali Zuo, Enqi Zhang1
1Otto-von-Guericke University , Magdeburg 39106 , Germany.
Researchers developed a novel nanoplatform using layered double hydroxide (LDH) nanoparticles. Angiopep-2 (Ang2) modification enhances brain targeting and delivery for treating brain diseases.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Neuroscience
Background:
- Developing effective drug delivery systems across the blood-brain barrier (BBB) is crucial for treating neurological disorders.
- Layered double hydroxide (LDH) nanoparticles offer potential as drug carriers but require targeted modifications for brain penetration.
Purpose of the Study:
- To design and evaluate a novel nanoplatform for enhanced brain targeting and delivery.
- To investigate the efficacy of Angiopep-2 (Ang2) and rabies virus glycoprotein (RVG) modified LDH nanoparticles for crossing the BBB.
Main Methods:
- Conjugation of LDH nanoparticles with Angiopep-2 (Ang2) or RVG targeting ligands via bovine serum albumin.
- In vitro assessment of nanoparticle delivery efficiency to brain endothelial cells (bEnd.3) and transcytosis through a simulated BBB model.
- In vivo confocal neuroimaging in rats and biodistribution studies in mice following intravenous administration.
Main Results:
- Ligand functionalization significantly improved LDH nanoparticle delivery to bEnd.3 cells and transcytosis across the BBB model.
- Ang2-modified LDH nanoparticles demonstrated enhanced and specific accumulation in the mouse brain compared to RVG-modified and unmodified LDH nanoparticles.
- In vivo imaging showed prolonged retention of peptide-ligand modified LDH nanoparticles in retinal vasculature.
Conclusions:
- Angiopep-2 (Ang2)-modified LDH nanoparticles represent a promising targeted nanoplatform for efficient brain drug delivery.
- The developed nanoplatform holds potential for the treatment of various brain diseases.
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