LAUSR

Caries is the most common chronic infectious disease in the human oral cavity and the existing anti-caries agents may lead to drug resistance and microecological imbalance. A novel urea derivative, 1,3-bis[3,5-bis(trifluoromethyl)phenyl]urea, has a potentially prominent antibacterial effect on cariogenic bacterial strain Streptococcus mutans UA159. In this study, we encapsulated the water-insoluble urea derivative in poly(lactic-co-glycolic acid) (PLGA) nanoparticles, performed physicochemical characterizations and explored its potential as a caries-preventive agent. The results showed that the drug-loaded PLGA nanoparticles exhibited satisfying surface morphology, particle size, size distribution and stability. With an optimized theoretical drug loading (10%), the drug-loaded PLGA nanoparticles exhibited negligible cytotoxicity against human oral squamous cell carcinoma cells. We noticed a biphasic drug release in vitro and the rate and cumulative release was higher in an acidic environment (pH 4.5) compared to a neutral environment (pH 7.4). The drug-loaded PLGA nanoparticles significantly inhibited the growth and lactic acid production of planktonic S. mutans as well as S. mutans biofilms. Our results indicate that the novel urea derivative-loaded PLGA nanoparticles serve as a promising anti-caries agent with remarkable pharmaceutical characteristics, low cytotoxicity, and satisfying antimicrobial effect.