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IN VITRO/IN VIVO PERFORMANCE STUDY OF NEW METRONIDAZOLE PERIODONTAL GEL FORMULATIONS

ADRIANA CIURBA¹, LUMINIȚA LAZĂR^2*, PAULA ANTONOAEA¹, ANCA MEDA GEORGESCU³, CAMIL-EUGEN VARI⁴, NICOLETA TODORAN¹

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The aim of this paper is to continue previous studies of gel formulation containing metronidazole and having mucoadhesive properties for the treatment of periodontal diseases by assessing their in vitro and in vivo characteristics. We started from the premise that the crosslink density and swelling capacity of the polyacrylic acid derivatives greatly affect the swelled mucoadhesive polymer which penetrates into the tissue crevices followed by the interpenetration between the polymer chains and protein chains of the mucus aimed to achieve correlations between the rheological properties of gels and mucoadhesivity. The results showed that the analysed gels F3_3, F3_1 (Ultrez 10) and F2_3 (Carbopol® 974P) have the most appropriate rheological properties. To evaluate the kinetics of drug release from the analysed gels, 9 kinetic models (functions of time) were performed. R2 adjusted (the adjusted coefficient of determination), MSC (model selection criterion) and AIC criterion (Akaike informational criterion) used as goodness of fit parameters indicated that Korsmeyer-Peppas is the most appropriate model to describe the release kinetics of the drug release from the 9 gel formulations. Preliminary clinical studies have shown that the topical application of metronidazole gel formulations, in combination with mechanical treatment of smoothening of the root surface appears to be more efficient, improving clinical parameters. Plaque index (PI), bleeding on probing index (BOP), and probing pocket depth (PPD) evaluated at one month post-treatment had better values compared with those of the initial examination values in a greater number of the periodontal examined sites (PI-54.15%, BOP-62.38%, and PPD- 28.45%) in the group B of patients receiving scaling and root planning (SRP) and 15% metronidazole gel formulation F3_3.