Effect of saccharin on antibacterial activity of chlorhexidine gel

Abstract

Although chlorhexidine is the most effective agent against dental plaque it is extremely bitter. To prepare formulations, it is necessary to use flavoring and sweetening, which can inhibit the antibacterial effect of chlorhexidine. Saccharin has been considered a compatible substance to use in chlorhexidine rinse or gel preparations; however, the effect of a range of concentrations has not been studied. To evaluate the effect of different concentrations of saccharin on the antibacterial activity of chlorhexidine gel, hydroxy-ethyl-cellulose gels containing 1.0% chlorhexidine digluconate and 0.0 to 1.0% sodium saccharin were prepared. Activity against Streptococcus mutans was evaluated using the agar diffusion method and determination of MIC values. The inhibitory zones of growth were 7.83 +/- 0.54 mm when no saccharin was added to the chlorhexidine gel and 7.75 +/- 0.50, 7.63 +/- 0.48, 6.21 +/- 0.40, 4.13 +/- 0.38, when the concentrations of saccharin in the gels were 0.02, 0.10, 0.5, and 1.0%, respectively. The range of MIC values was 1-2 micrograms/ml, with saccharin concentrations of 0%, 0.02, and 0.1%. In contrast, the MIC values were 4-8 and 8-16 micrograms/ml with saccharin concentrations of 0.5% and 1.0%, respectively. The paired "t" test showed that 0.5 and 1.0% sodium saccharin inhibit the antibacterial activity of 1% digluconate chlorhexidine gel. These in vitro results suggest that saccharin may inhibit the efficacy of chlorhexidine against mutans streptococci, depending on the concentration.Although chlorhexidine is the most effective agent against dental plaque it is extremely bitter. To prepare formulations, it is necessary to use flavoring and sweetening, which can inhibit the antibacterial effect of chlorhexidine. Saccharin has been considered a compatible substance to use in chlorhexidine rinse or gel preparations; however, the effect of a range of concentrations has not been studied. To evaluate the effect of different concentrations of saccharin on the antibacterial activity of chlorhexidine gel, hydroxy-ethyl-cellulose gels containing 1.0% chlorhexidine digluconate and 0.0 to 1.0% sodium saccharin were prepared. Activity against Streptococcus mutans was evaluated using the agar diffusion method and determination of MIC values. The inhibitory zones of growth were 7.83 +/- 0.54 mm when no saccharin was added to the chlorhexidine gel and 7.75 +/- 0.50, 7.63 +/- 0.48, 6.21 +/- 0.40, 4.13 +/- 0.38, when the concentrations of saccharin in the gels were 0.02, 0.10, 0.5, and 1.0%, respectively. The range of MIC values was 1-2 micrograms/ml, with saccharin concentrations of 0%, 0.02, and 0.1%. In contrast, the MIC values were 4-8 and 8-16 micrograms/ml with saccharin concentrations of 0.5% and 1.0%, respectively. The paired "t" test showed that 0.5 and 1.0% sodium saccharin inhibit the antibacterial activity of 1% digluconate chlorhexidine gel. These in vitro results suggest that saccharin may inhibit the efficacy of chlorhexidine against mutans streptococci, depending on the concentration1112934Embora clorexidina seja reconhecida como o agente antimicrobiano mais eficiente contra placa dental, seu gosto extremamente amargo é uma limitação nos preparos farmacêuticos. Substâncias adoçantes e flavorizantes usadas para preparar formulações podem inibir a atividade antibacteriana da clorexidina. Sacarina tem sido considerada uma substância compatível para ser usada em enxaguatórios bucais ou géis, entretanto o efeito da concentração deste adoçante não tem sido estudado. A atividade antibacteriana de géis de clorexidina a 1%, contendo sacarina de 0,0 a 1,0%, foi avaliada a partir de preparações farmacêuticas formuladas. Atividade contra Streptococcus mutans foi avaliada através da inibição do crescimento em ágar e determinação da concentração inibitória mínima (CIM). Os halos de inibição de crescimento foram de 7,83 ± 0,54 mm, na ausência de sacarina, e de 7,75 ± 0,50, 7,63 ± 0,48, 6,21 ± 0,40 e 4,13 ± 0,38 quando da presença de sacarina a 0,02, 0,10, 0,5 e 1%, respectivamente, nos géis de clorexidina a 1%. A faixa de CIM foi de 1-2 µg/ml quando da presença de 0,0, 0,02 e 0,1% de sacarina nos géis. Quando o gel de clorexidina a 1% continha sacarina a 0,5 e 1% a CIM foi de 4-8 e 8-16 µg/ml, respectivamente. Teste "t" pareado mostrou que sacarina sódica nas concentrações de 0,5 e 1% inibiu a atividade anti mutans de digluconato de clorexidina a 1% em gel. Estes resultados in vitro sugerem que sacarina pode inibir a eficácia de clorexidina contra streptococcus do grupo mutans, dependendo da concentração usad

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