In Vitro Evaluation of Seven Cationic Detergents as Antiplaque Agents

Abstract

The bactericidal efficacy of seven cationic detergents was studied in vitro against intact preformed plaques of representative strains of four oral dental plaque-forming microorganisms: Streptococcus mutans, Streptococcus sanguis, Actinomyces viscosus, and Actinomyces naeslundii. Both absolute (plaque bactericidal index) and relative (chlorhexidine coefficient) indexes of antiplaque activity were established. Only cetyltrimethylammonium bromide was more efficacious than the reference agent, the bisbiguanide chlorhexidine, for the apparently more potent tooth-adherent cariogenic and periodontopathic elements, respectively, of the in vivo plaque microflora, S. mutans and A. viscosus.Control Qf dental plaque, which is associated with gingivitis and dental caries, may be achieved by topical applications of antimicrobial agents (11,18,19). Topical rather than systemic administration of such agents to supragingival plaque is indicated because of its dense, toothadherent nature and, importantly, because plaque is not bathed in blood or interstitial fluids but is exposed to the environment of the oral cavity.Cationic detergents have been known for a number of years to possess bactericidal and fungicidal properties (17). Cationic agents are also of interest because of potential reversible binding (substantivity) to anionic groups on oral mucous membranes (2,21,22,25,26), which could permit possible prolonged intraoral retention and sustained release of such cationic antiseptics. Recent studies have demonstrated modest in vivo and in vitro antiplaque activities of three quaternary ammonium detergents, namely, cetylpyridinium chloride, domiphen bromide, and benzylalkonium chloride (1,6,12,27,35). In those studies, however, the optimal conditions required for in vivo efficacy were not evaluated.In the work reported herein an examination of seven cationic detergents was undertaken with a view to establishing the optimal conditions likely to achieve maximal efficacy in vivo. These agents were assessed for their antiplaque activities against strains of four oral plaqueforming microorgansms by using an in vitro preformed-plaque model system (30, 31), and their potencies were compared on both absolute t Present address:

In vitro activity of A-16686, a potential antiplaque agent

“…Other agents, such as CHX and other cationic compounds, are more extensively employed in various formulations (2,3,5,6,17). These compounds showed good bactericidal activity by reducing cariogenic bacteria and good antiplaque activity (2,15,24,25). For these reasons, CHX, BKC, and CPC were selected for comparison with A-16686.…”

6-Hydroxyquinolinium salts differing in the length of alkyl side-chain: Synthesis and antimicrobial activity

“…6-hydroxyquinolinium derivative (8) showed the exact same efficacy as its N-benzalkonium analogue (B 12 ) against G+ strains, whereas P 12 exerted substantially lower efficacy except against SA and SE where the efficacy was similar to 8 and B 12 . As regards the length of alkyl chain, no clear trend has been observed.…”

“…5 N-Alkylpyridinium quaternary compounds are often used in analytical chemistry as auxiliary solubilizers of water-insoluble substances, 6 or for instance, as antiplaque agents in chewing gums. 7,8 Moreover, these compounds are known for their competitive inhibitory activity on acetylcholinesterase 9 and antagonistic effect on nicotinic receptors. 10 With respect to the capability to form an interface between polar and non-polar phases, the use of N-alkylpyridinium salts as carriers to improve absorption of oligonucleotides through the cellular phospholipid membrane has been described.…”

“…Yields, melting points, retention times and Clog P of prepared 6-hydroxyquinolinium salts(7)(8)(9)(10)(11). The retention times were determined by isocratic (the first value) and gradient elution (the second value).b Clog P were calculated in HyperChem 7.52 according to the method of Ghose, Pritchett and Crippen.…”

Antimicrobial activity of N,N'-dialkylpolymethylenediamines against some dental plaque bacteria

“…Among these agents, chlorhexidine, a bisbiguanide compound, has been shown to exert antimicrobial and/or antiplaque effects (10). In addition, some cationic detergents such as cetylpyridinium chloride have been investigated for the same purpose (1,11). N,N'-Dialkylpolymethylenediamines, a group of cationic detergents, have been mainly regarded as additives for use as metal chelate surfactants (7).…”