Single-step surface functionalization of polymeric nanoparticles for targeted drug delivery

Area of Science:

• Nanotechnology
• Materials Science
• Biomedical Engineering

Background:

• Targeted drug delivery relies on nanocarrier surface functionalization with ligands.
• Current methods are inefficient, multi-step, and limit multi-ligand incorporation.

Purpose of the Study:

• To develop a versatile, single-step surface functionalization technique for polymeric nanoparticles.
• To enable simultaneous incorporation of multiple targeting ligands onto nanocarriers.

Main Methods:

• Utilized a diblock copolymer (polylactide-polyethylene glycol) in nanoparticle formulation.
• Employed a one-pot approach with PLA-PEG-ligand conjugates for surface functionalization.
• Confirmed ligand incorporation using NMR, SPR, TEM, and cell uptake studies.

Main Results:

• Successfully achieved simultaneous functionalization with biotin and folic acid on drug-loaded nanoparticles.
• Demonstrated enhanced nanoparticle accumulation in tumors in vivo.
• Showed significantly improved efficacy of paclitaxel-loaded nanoparticles in a mouse xenograft model.

Conclusions:

• The developed IAASF approach offers a versatile and efficient method for multi-ligand nanoparticle functionalization.
• This technique facilitates the development of advanced targeting strategies for various tissues.
• Enables enhanced therapeutic outcomes through multi-ligand targeted drug delivery.