Bioavailability and cytotoxicity of dihydroquercetin – L-lysine compositions

Authors:
Publisher website
Google Scholar
Abstract
Introduction. Dihydroquercetin (DHQ) is a natural flavanonol with a high safety profile and various biological effects. Among these, anti-inflammatory and wound-healing properties stand out. However, one of the challenges in developing drugs based on DHQ is its limited solubility in water at room temperature, which affects its bioavailability. This makes it difficult for DHQ to be used in medicine. Objective: to investigate the biopharmaceutical properties and cytotoxicity of DHQ compositions in combination with L-lysine. Material and methods. To obtain DHQ compositions with L-lysine, the following steps were taken: first, the material was ground, then lyophilized or dried in an aqueous solution at 65°C. The solubility of the resulting product was assessed in accordance with the GPA.1.2.1.0005 of the Russian Federation State Pharmacopoeia XV and the EAEU Pharmacopoeia. A method for quantitative analysis of flavonoids in a mechanical mixture was developed based on UV-spectrophotometry. The bioavailability of the compound was assessed by its diffusion into agar, and its cytotoxic properties were tested on CaCo-2, 3T3, HUVEC, and HEK293 cell lines in experimental conditions using CCK-8. Results. A mechanical mixture with significantly improved solubility compared to the original flavonoid was produced using the grinding method. The resulting compositions, in the form of lyophilizates and films, have similar solubility, classified as "very easily soluble" according to Russian Federation State Pharmacopoeia XV. A significant increase in bioavailability was observed as a result of these compositions. A method for quantifying flavonoids using UV-spectrophotometry was developed. When studying the cytotoxic properties of these objects, it was found that lyophilization reduced cytotoxicity, with IC50 values of 0.025, 0.068, 0.145 and 0.288 mg/ml for 3T3, HEK293, CaCo-2, and HUVEC cells, respectively. Conclusion. The obtained modifications may be interesting from the point of view of increasing the bioavailability and solubility of natural flavonoids. This solves one of the main problems in the development of drug products based on these compounds

This publication has 13 references indexed in Scilit: