Fucoidan-Functionalized Nanoparticles for Antimycobacterial Therapy: A Promising Approach against Drug-Resistant...

Area of Science:

• Nanotechnology
• Infectious Diseases
• Pharmacology

Background:

• Tuberculosis (TB) remains a significant global health threat, driven by Mycobacterium tuberculosis (Mtb).
• Multidrug-resistant TB (MDR-TB) presents a critical challenge, necessitating novel therapeutic strategies.
• Existing treatments face limitations in efficacy and targeted delivery.

Purpose of the Study:

• To develop and evaluate fucoidan-coated poly-(isobutyl cyanoacrylate) (PIBCA) nanoparticles as a targeted delivery system for rifampicin (RIF).
• To assess the efficacy of these nanoparticles against both drug-sensitive and drug-resistant Mtb strains.
• To investigate the cellular uptake and intracellular bactericidal activity of the RIF-loaded nanoparticles.

Main Methods:

• Anionic emulsion polymerization was used to synthesize PIBCA nanoparticles.
• Nanoparticles were characterized for size, zeta potential, morphology, and colloidal stability.
• In vitro antimycobacterial activity, cytotoxicity, cellular uptake, and synergistic effects were evaluated.

Main Results:

• PIBCA nanoparticles exhibited a mean diameter of 400-480 nm, negative zeta potential, and good colloidal stability.
• High encapsulation efficiency (40-50%) for rifampicin was achieved.
• Nanoparticles demonstrated significant antimycobacterial activity against sensitive (MIC: 0.412 μg/mL) and resistant (MIC: 1.238 μg/mL) strains with low cytotoxicity.
• Efficient cellular uptake and intracellular bactericidal activity were observed, mediated by fucoidan targeting of macrophage receptors.

Conclusions:

• Fucoidan-coated PIBCA nanoparticles represent a promising nanocarrier for rifampicin delivery.
• This strategy enhances drug efficacy against Mycobacterium tuberculosis, particularly MDR-TB strains.
• The targeted delivery mechanism improves intracellular drug concentration and bactericidal activity within macrophages.