Bioavailability and cytotoxicity of dihydroquercetin – L-lysine compositions
- Authors: Svotin A.A.1, Korochkina M.D.1, Kolesnikova D.R.1, Krivosheeva E.A.1, Terekhov R.P.1, Selivanova I.A.1
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Affiliations:
- Sechenov First Moscow State Medical University (Sechenov University)
- Issue: Vol 74, No 8 (2025)
- Pages: 31-39
- Section: Pharmaceutical chemistry and pharmacognosy
- URL: https://journal-vniispk.ru/0367-3014/article/view/365717
- DOI: https://doi.org/10.29296/25419218-2025-08-04
- EDN: https://elibrary.ru/iqgzvf
- ID: 365717
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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.
About the authors
Artem Aleksandrovich Svotin
Sechenov First Moscow State Medical University (Sechenov University)
Author for correspondence.
Email: svotin_a_a@staff.sechenov.ru
ORCID iD: 0009-0001-5360-8816
Assistant Professor, Department of Chemistry of Nelyubin Institute of pharmacy
Russian Federation, Trubetskaya str., 8/2, Mosсow, 119048Maria Dmitrievna Korochkina
Sechenov First Moscow State Medical University (Sechenov University)
Email: korochkina_m_d@student.sechenov.ru
ORCID iD: 0000-0002-2790-9041
Student, Nelyubin Institute of pharmacy
Russian Federation, Trubetskaya str., 8/2, Mosсow, 119048Diana Romanovna Kolesnikova
Sechenov First Moscow State Medical University (Sechenov University)
Email: kolesnikova_d_r@student.sechenov.ru
ORCID iD: 0009-0002-4447-7225
Postgraduate Student, Department of pharmaceutical technology of Nelyubin Institute of pharmacy
Russian Federation, Trubetskaya str., 8/2, Mosсow, 119048Elizaveta Andreevna Krivosheeva
Sechenov First Moscow State Medical University (Sechenov University)
Email: krivosheeva_e_a@student.sechenov.ru
ORCID iD: 0009-0001-6639-9400
Student, Nelyubin Institute of pharmacy
Russian Federation, Trubetskaya str., 8/2, Mosсow, 119048Roman Petrovich Terekhov
Sechenov First Moscow State Medical University (Sechenov University)
Email: terekhov_r_p@staff.sechenov.ru
ORCID iD: 0000-0001-9206-8632
Candidate of Pharmaceutical Sciences, Associate Professor, Department of Chemistry of Nelyubin Institute of pharmacy
Russian Federation, Trubetskaya str., 8/2, Mosсow, 119048Irina Anatolyevna Selivanova
Sechenov First Moscow State Medical University (Sechenov University)
Email: selivanova_i_a@staff.sechenov.ru
ORCID iD: 0000-0002-2244-445X
Doctor of Pharmaceutical Sciences, Professor, Professor, Department of Chemistry of Nelyubin Institute of pharmacy
Russian Federation, Trubetskaya str., 8/2, Mosсow, 119048References
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