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DOI: 10.1055/s-0043-1774274
Enhancement of luteolin solubility in carriers and drug delivery systems and formulation of a toothpaste with luteolin for periodontal diseases
Luteolin (LUT) is a naturally derived bioactive flavonoid with significant anti-microbial and anti-inflammatory properties. The physicochemical properties of luteolin, such as its very high melting point (601 – 614 K) and its very low solubility in water, are mainly due to the strong intermolecular forces. LUT shows significant formulation problems due to its poor aqueous solubility and water stability [1]. In order to use LUT as an active ingredient in gels/toothpastes for periodontal applications, we aimed, in the frame of the project LuteoPaste, to initially enhance solubility of LUT in several carriers and overcome such limitations for product development and subsequently to incorporate that in the final formulation.
Specifically, solubilisation of LUT in lipophilic flavours used in toothpastes and gels, as well as in micelles by the use of non-ionic surfactants, such as PEG derivatives, was examined. Furthermore, drug delivery systems (DDS) of varying concentrations of LUT were prepared, such as liposomes, complexes with cyclodextrins and chitosan. Following the successful solubilisation of LUT into several carriers and DDS, different combinations of excipients (gelling agent, thickener, dispersing agent, humectant, polishing agent, opacifier etc.) at varying concentrations, were utilized to formulate a toothpaste for periodontitis with LUT as active ingredient, that will be used for further in vivo studies in dogs. Stability of the developed toothpastes/gels was examined and scale up characteristics have been defined.
Funding This research has been co-financed by the European Regional Development Fund of the European Union and Greek national funds through the Operational Program Competitiveness, Entrepreneurship and Innovation, under the call RESEARCH – CREATE – INNOVATE (project code: T2EDK-01627).
Publikationsverlauf
Artikel online veröffentlicht:
16. November 2023
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References
- 1 Peng B, Yan W.. Solubility of luteolin in ethanol+water mixed solvents at different temperatures. J Chem Eng Data 2010; 55: 583-585