Development of Thermoreversible Dental Gel with Berberine

Abstract

Introduction. Dental gel is one of the modern dosage forms with optimal biopharmaceutical properties for the treatment and prevention of oral diseases An isoquinoline alkaloid berberine is the promising active substance with antibacterial and anti-inflammatory effect, capable of forming stable dispersed systems with gel-forming components. It is noteworthy that, despite the pronounced antimicrobial activity of the alkaloid berberine, there is currently no dental dosage form with this component on the pharmaceutical market, and therefore research in this direction is of great interest.Aim. Selection of the optimal technology for obtaining dental gel with berberine for the treatment of oral diseases.Materials and methods. Berberine bisulfate (manufactured by CJSC «Vifitech», Obolensk, Moscow region, RF), poloxamers P407 and P338 (EP, USP/N; BASF, Germany), propylene glycol (USP; BASF, Germany), sodium chloride (Sigma-Aldrich, Germany, Cat. No. S9888), mucin type II from a pig stomach (Sigma-Aldrich, Germany, Cat. No. M2378). In the development of the composition and technology for the preparation of gels, a magnetic stirrer with a temperature control function (C-MAG HS 7 from IKA, Germany) was used. Gels were prepared by the «hot method» and «cold method».Results and discussion. The production of the gel by the «hot method» provided a uniform dosage form. The obtained pH value is within the range of optimal diapason. Measurement of the specific peel force of the model gel sample showed pronounced mucoadhesive properties, which indicates that there is no need to adjust this parameter by introducing additional components into the formulation. The spectroscopic method is applicable for the analysis of berberine gel. It has been found that a significant dilution of the reference substance sample is required to develop an identification procedure.Conclusion. The production of a sample of the dosage form by the «hot method» is optimal, which is probably due to the effect of solubilization and better distribution of the active substance in the base.

Spray Film-Forming systems as promising topical in situ Systems: A review

“…It is important to note that measuring methods for mucoadhesive properties are insufficiently described in studies devoted to the development of spray film-forming systems ( Kathe and Kathpalia, 2017 ; Gohel and Nagori; Bakshi et al, 2008 , Kirzhanova et al, 2014 , Queen et al, 1987 ). At the same time, at least a dozen reproducible validated methods for determining this indicator are currently known, including both in vivo , ex vivo , and in vitro methods ( Kirzhanova et al, 2014 , Palvinskiy et al, 2020 ). The profitability of in vivo studies of mucoadhesion may be high for the motivation of the authors to conduct full-fledged studies in this area.…”