IN-VITRO AND IN-VIVO STUDIES ON SALIFLUOR PVM/MA COPOLYMER/NAF COMBINATION AS AN ANTIPLAQUE AGENT/

Salifluor (5-n-octanoyl-3'-trifluoromethyl-salicylanilide), a broad sp ectrum antimicrobial agent, was investigated for its ability to inhibi t dental plaque formation. A combination of salifluor with PVM/MA copo lymer and NaF was optimized for its antiplaque effect in mouthrinse an d dentifrice formulations based on a series of both laboratory and cli nical studies. It was found that salifluor, a highly hydrophobic compo und, could not be adequately solubilized with the conventional amount of sodium lauryl sulfate (SLS), the most commonly used anionic surfact ant in oral hygiene products. However, it was possible to prepare stab le mouthrinse formulations using a mixed surfactant system containing both anionic and nonionic surfactants. The most suitable mixture was f ound to be a combination of SLS, Pluronic and Tauranol in a proportion of 1:1:1. This combination provided adequate stability and high antim icrobial activity as determined by in vitro microbiological tests. Add ition of a PVM/MA copolymer to the formulation improved the adsorption and retention of salifluor on simulated tooth surfaces In vitro (sali va coated hydroxyapatite disks) by almost two-fold and also increased the antiplaque efficacy in both laboratory and human clinical studies. It was also found that a non fluoride dentifrice containing a combina tion of salifluor and PVM/MA copolymer with a dicalcium phosphate dihy drate abrasive, was highly effective in reducing smooth surface and fi ssure caries in rats. The results of the present studies demonstrated that salifluor is an effective anti-plaque agent in mouthrinse and den tifrice when carefully formulated to maximize its delivery and bioavai lability on oral surfaces. They also illustrated the difficulties enco untered in exploiting the antimicrobial efficacy of highly hydrophobic , nonionic antimicrobial agents such as salifluor in commonly used ora l hygiene vehicles.