Multifunctional Neomycin-Triazine-Based Cationic Lipids for Gene Delivery with Antibacterial Properties

Area of Science:

• Biomaterials Science
• Gene Therapy
• Antimicrobial Research

Background:

• Cationic lipids (CLs) are key nonviral gene delivery vectors.
• There is a growing need for multifunctional CLs with both gene delivery and antibacterial capabilities.

Purpose of the Study:

• To design and synthesize novel aminoglycoside (AG)-based multifunctional vectors.
• To evaluate their gene transfection efficiency and antibacterial properties.

Main Methods:

• Cationic amphiphiles were synthesized on a triazine scaffold, functionalized with neomycin (Neo) as the polar head and various lipophilic tails (stearyl, oleyl, cholesteryl).
• DNA condensation, cell transfection, cytotoxicity, and antibacterial activity were evaluated for the synthesized CLs.

Main Results:

• Neo-triazine-based CLs showed excellent DNA condensation ability at low charge ratios.
• Derivatives exhibited strong transfection performance with negligible cytotoxicity across two cell lines.
• CLs with symmetric two-tailed oleyl (OL) were most effective for transfection.
• Neo-triazine-based derivatives displayed significant antibacterial activity against Gram-negative bacteria, particularly those with one or two aliphatic chains.

Conclusions:

• Neo-triazine-based derivatives are effective multifunctional nonviral gene delivery vectors.
• These compounds possess both high transfection efficiency and notable antibacterial properties, highlighting their therapeutic potential.