Novel Cationic Amphiphiles Control Biofilm Formation for Bacterial Vaginosis

Cationic amphiphiles greatly inhibits the biofilm formation of the pathogenic bacteria in BV. Cationic Amphiphile Concentration (μM)

Invention Summary:

Bacterial vaginosis (BV) is a common polymicrobial infection in women of reproductive age, affecting 10-30% of women in developed nations. BV can lead to serious complications such as abortion, premature birth  and pelvic inflammatory disease. Current antibiotic treatment regimens often fail to fully eradicate the pathogenic biofilm and may lead to recurrance due to antibiotic resistence. Antimicrobial peptides (AMPs) hold great potential in treating BV as they can effectively disrupt the bacterial membrane causing cell death, a mechansim that is difficult for bacteria to develop drug resistance to. However, intrinsic drawbacks associated with AMPs, such as low metabolic stability (i.e., susceptibility to proteolysis), high manufacturing cost and formulation difficulties have precluded their translation into clinical arena.

Rutgers scientists have developed two series of cationic amphiphiles (CAms) that chemically mimic AMPs. Compared to AMPs, these ether- and ester-linked CAms showed higher stability and solubility, high biodegradability, and good efficacy against various gram-positive and gram-negative bacteria. In an in vitro study, the CAms were shown to effectively inhibit BV-associated pathogens but not the healthy vaginal bacteria lactobacilli. Using the biofilm crystal violet staining assay, the CAms were shown to strongly inhibit the biofilm formation of the BV pathogenic bacteria with µM activities and are much tolerated by the healthy bacteria lactobacilli.

In addition, CAms also display synergistic effects when used in combination with metronidazole, a commonly used antibiotic to treat BV. Furthermore, scanning electron microscopy (SEM) revealed considerable morphological and ultrastructural changes in treated biofilms, confirming the membrane-targeting effects of CAms.  These results suggest CAms are a promising new generation of antimicrobials for treating bacterial vaginosis.

Market Applications:

• Novel therapeutics to treat BV.
• Novel combination therapeutics with metronidazole to treat BV.
• Additives in personal care products to prevent or treat BV.

Advantages:

• Capable of eradicating pathogenic biofilms
• Strong antimicrobial effects with µM activity
• Unlikely to result in resistance due to its membrane-disruption mechanism
• Well-tolerated by the healthy vaginal bacteria lactobacilli
• Highly versatile chemistry with potential for improvement
• Biocompatible, biodegradable and eco-friendly

Intellectual Property & Development Status:

Patent issued. Available for licensing and/or research collaboration.