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Cyclodextrin enhanced antimicrobial efficiency of triclosan against Streptococcus mutans

The dental plaque control is an important step in prevention and treatment of dental diseases, such as caries, gingivitis and peridontitis. This might be achieved by regular brushing supported by the use of a suitable antimicrobial agent, such as triclosan. Although triclosan shows a potent activity against Streptoccocus mutans, S. sanguis, S. salivarius and Actinoyicetes species, which have a major role in aetiology of dental conditions, therapeutical efficiency of this compound is significantly impaired by its practical insolubility in water. The aim of this work was to improve triclosan aqueous solubility, and consequently its antimicrobial activity, through drug complexation with parent β-cyclodextrin (βCD) and its water-soluble polymeric derivative (PβCD). The particular goal was to monitor the effect of cyclodextrin complexation on the antimicrobial activity of the drug both as such or formulated as in situ cross-linking mucoadhesive buccal patch, using S. mutans ATCC 33402 as a model for the evaluation of the triclosan therapeutic efficacy. Triclosan complexes with βCD and PβCD, prepared by co-grinding in a high energy vibrational micromill, increased triclosan solubility in simulated saliva of 9.6 and 21 times, respectively. When monitored as a function of time, antimicrobial activity of triclosan complexes against S. mutans was superior to that of pure compound, which in 24 h reduced the number of bacteria for only 2 log10CFUmL-1. In this same time both complexes completely eradicated S. mutans, and efficiency of TR/PβCD in first 4 h was superior to that of TR/βCD, in agreement with their different solubilities. Similar effects were observed when the drug, alone or as cyclodextrin complexes was loaded into buccal patches formulated with low methoxy amidated pectin (AMP) and carbomer (CAR). Preliminary studies showed that patches formulated with 80:20 w/w AMP:CAR mixture showed suitable swelling properties, low erosion (20.6%), and good mucoadhesion. In vitro dissolution studies supported by antimicrobial studies clearly demonstrated the superior performance of patch formulations loaded with cyclodextrin complexes. In fact, TR/PβCD loaded formulation showed an inhibition zone of 51.0±1.3 mm, which was comparable to that of ampicilin control (48.0±5.3 mm), clearly demonstrating the good therapeutic potential of the developed formulation in eradication of S. mutans.

triclosan; cyclodextrin; Streptococcus mutans

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