Liposomal Vancomycin-Cefazolin Nanoparticle for Treating Infections

A novel liposomal nanoparticle delivering vancomycin and cefazolin enhanced with targeting ligands improves treatment efficacy of Staphylococcus aureus infections, including MRSA, while reducing kidney toxicity.  

Technology Summary

“Methicillin-resistant Staphylococcus aureus (MRSA) represents one of the most significant antimicrobial resistance challenges in global health, responsible for approximately 90% of S. aureus infections.” Using nanoparticles to delivering highly concentrated drugs directly to the infection site leads to reduced toxicity and effective treatment while overcoming antibiotic resistance.

This technology comprises a liposomal nanoparticle drug delivery system encapsulating vancomycin and cefazolin manufactured via a modified water-in-oil reverse phase evaporation and high-pressure homogenization method that leads to optimized drug-to-lipid ratios suitable for or in vivo delivery. The nanoparticles are decorated with ligands such as folate to specifically target folate receptor-expressing infected tissues caused by Staphylococcus aureus, including methicillin-resistant strains (MRSA). The folate-targeted liposomes exhibit enhanced bactericidal activity, improved tissue penetration, controlled drug release, biofilm inhibition, and reduced accumulation in off-target organs like kidneys, thereby lowering potential nephrotoxicity.

Key Advantages

• High drug loading efficiency of water-soluble antibiotics in liposomes
• Nanoscale uniform particle size for optimal tissue penetration and circulation
• Enhanced accumulation and retention at infection sites through folate receptor targeting
• Reduced nephrotoxicity by lowering drug accumulation in kidneys
• Versatile targeting ligands enabling cell-specific delivery (leukocytes, fibroblasts, bacterial cells)

Market Opportunities

• Overcomes antibiotic resistance and reduced efficacy of conventional vancomycin therapy for MRSA
• Minimizes nephrotoxicity associated with high-dose vancomycin treatments
• Improved bactericidal efficacy and biofilm inhibition compared to free antibiotics
• Potential expansion to other bacterial infections using targeted liposomal antibiotics

Stage of Development

Pre-Clinical

Patent Status

US Issued Patent 12,551,527 "DRUG DELIVERY SYSTEMS FOR TREATMENT OF INFECTIONS"

References & Publications

“Folate Functionalized Lipid Nanoparticles for Targeted Therapy of Methicillin-Resistant Staphylococcus aureus” DOI: 10.3390/pharmaceutics13111791

“Impact of cefazolin co-administration with vancomycin to reduce development of vancomycin-intermediate Staphylococcus aureus”
DOI: 10.1016/j.diagmicrobio.2018.03.020