Transferrin- and folate-modified, double-targeted nanocarriers for gene delivery

Area of Science:

• Biomedical Engineering
• Nanotechnology
• Gene Therapy

Background:

• Nanocarrier surface modification with ligands enhances targeting and internalization into specific cells like cancers.
• Ligand-receptor interactions are crucial for targeted delivery and cellular uptake.

Purpose of the Study:

• To develop systemically administrable nanocarriers modified with dual ligands (transferrin and folate).
• To enhance receptor-mediated targeting and nuclear uptake of genetic materials for improved gene delivery.

Main Methods:

• Transferrin (Tf) and folate (Fa) were conjugated to polyethylene glycol-phosphatidylethanolamine (PEG-PE).
• Dual-ligand modified (D-modified) vectors were created using T-PEG-PE and F-PEG-PE.
• In vivo transfection efficiency was evaluated in tumor-bearing animal models.

Main Results:

• D-modified solid lipid nanoparticles/enhanced green fluorescence protein plasmid (D-SLN/pEGFP) had a particle size of 226 nm and 90% gene loading.
• D-SLN/pEGFP demonstrated over 30% higher transfection efficiency compared to unmodified and single-ligand modified SLN/pEGFP in HepG2 cells.

Conclusions:

• Transferrin and folate act as effective active targeting ligands, improving nanocarrier cell-targeting capabilities.
• The developed dual-ligand modified vectors represent a promising active targeting gene delivery system.