Screening study of the antihyperglycemic action of new solid quercetin dispersions
DOI:
https://doi.org/10.15587/2519-4852.2021.247443Keywords:
quercetin, solid dispersion, hydroxypropyl methylcellulose, polyvinylpyrrolidone, diabetes mellitus, screening, antihyperglycemic actionAbstract
The aim – to screen new solid dispersions of quercetin for the presence of antihyperglycemic action and to identify the most active substances that are promising for the creation of antidiabetic drugs.
Materials and methods. The object of the study was 4 new solid dispersions of quercetin, developed at the National University of Pharmacy. Solid dispersions of quercetin were prepared by the liquid-phase method; hydroxypropyl methylcellulose (HPMC) or polyvinylpyrrolidone (PVP) in ratios of 1:1 and 1:2 were used as a carrier. The antihyperglycemic effect of the studied substances at a dose of 50 mg / kg was assessed in rats by the ability to lower blood glucose levels after carbohydrate loading in a model of impaired glucose tolerance induced by dexamethasone and in experimental type 2 diabetes mellitus induced by dexamethasone.
Results. It was found that with impaired glucose tolerance, a solid dispersion of quercetin with HPMC (1:1) showed a pronounced antihyperglycemic effect – the glucose level 30 minutes after glucose load significantly decreased by 28 % and did not differ from the action of metformin, which was confirmed by the value of the area under glycemic crooked. When solid dispersions with PVP (1:1 and 1:2) were used, the antihyperglycemic effect was less pronounced. In a model of type 2 diabetes mellitus, a significant antihyperglycemic effect was found only in a solid dispersion of quercetin with HPMC (1:1) at the metformin level, which indicates an increase in the solubility and absorption of quercetin.
Conclusions. A pronounced antihyperglycemic effect at the metformin level was found in a solid dispersion of quercetin with HPMC in a 1:1 ratio with impaired glucose tolerance and type 2 diabetes mellitus. It has been proven that a solid dispersion of quercetin with HPMC is a promising substance for creating a monocomponent drug or for inclusion in a new antidiabetic combined drug
References
- International diabetes federation Diabetes Atlas. Available at: http://www.diabetesatlas.org
- Dedov, I. I., Shestakova, M. V., Mayorov, A. Y., Vikulova, O. K., Galstyan, G. R., Kuraeva, T. L. et. al. (2017). Standards of specialized diabetes care. Edited by Dedov II, Shestakova MV, Mayorov AY. 8th edition. Diabetes Mellitus, 20 (1S), 1–121. doi: http://doi.org/10.14341/dm20171s8
- Unuofin, J. O., Lebelo, S. L. (2020). Antioxidant Effects and Mechanisms of Medicinal Plants and Their Bioactive Compounds for the Prevention and Treatment of Type 2 Diabetes: An Updated Review. Oxidative Medicine and Cellular Longevity, 2020, 1–36. doi: http://doi.org/10.1155/2020/1356893
- Pang, G.-M., Li, F.-X., Yan, Y., Zhang, Y., Kong, L.-L., Zhu, P. et. al. (2019). Herbal medicine in the treatment of patients with type 2 diabetes mellitus. Chinese Medical Journal, 132 (1), 78–85. doi: http://doi.org/10.1097/cm9.0000000000000006
- Savka, I. I., Savka, T. B. (2020). Mechanisms of Macro-, Micro- and Ultramicroscopic Transformation of Bodies in Type 2 Diabetes. Ukrainian Journal of Medicine, Biology and Sport, 5 (2), 36–42. doi: http://doi.org/10.26693/jmbs05.02.036
- Sharafetdinov, K. K., Plotnikova, O. A., Pilipenko, V. V., Nikitjuk, D. B. (2020). Oxidative stress and increasing antioxidant defence in type 2 diabetes. Clinical Nutrition and Metabolism, 1 (3), 127–136. doi: http://doi.org/10.17816/clinutr50340
- Tarakhovskii, Iu. S., Kim, Iu. A., Abdrasilov, B. S., Muzafarov, E. N. (2013). Flavonoidy: biokhimiia, biofizika, meditsina. Puschino: Sunchrobook, 310.
- Shi, G.-J., Li, Y., Cao, Q.-H., Wu, H.-X., Tang, X.-Y., Gao, X.-H. et. al. (2019). In vitro and in vivo evidence that quercetin protects against diabetes and its complications: A systematic review of the literature. Biomedicine & Pharmacotherapy, 109, 1085–1099. doi: http://doi.org/10.1016/j.biopha.2018.10.130
- Riva, A., Ronchi, M., Petrangolini, G., Bosisio, S., Allegrini, P. (2018). Improved Oral Absorption of Quercetin from Quercetin Phytosome®, a New Delivery System Based on Food Grade Lecithin. European Journal of Drug Metabolism and Pharmacokinetics, 44 (2), 169–177. doi: http://doi.org/10.1007/s13318-018-0517-3
- Chen, X., McClements, D. J., Zhu, Y., Chen, Y., Zou, L., Liu, W. et. al. (2018). Enhancement of the solubility, stability and bioaccessibility of quercetin using protein-based excipient emulsions. Food Research International, 114, 30–37. doi: http://doi.org/10.1016/j.foodres.2018.07.062
- Kononenko, N. M., Ruban, O. A., Chikitkina, V. V., Kovalevska, I. V. (2020). The influence of antidiabetic combined medicinal product glik verin based on voglibose and quercetin on lipid e xchange indices under conditions of experimental metabolic syndrome. Problems of Endocrine Pathology, 74 (4), 124–130. doi: http://doi.org/10.21856/j-pep.2020.4.16
- Kovalevska, I. V., Ruban, E. A., Kutsenko, S. A., Kutova, O. V., Kovalenko, Sv. M. (2017). Study of physical and chemical properties of solid dispersions of quercetin. Asian Journal of Pharmaceutics, 11 (4), 805–809.
- Stefanova, O. V. (Ed.) (2001). Doklinichni doslidzhennia likarskykh zasobiv. Kyiv: Avitsenna, 528.
- Kovalevska, I., Ruban, O. (2018). Development of the methodological approach of obtaining preparations based on solid dispersions. ScienceRise: Pharmaceutical Science, 4 (14), 4–8. doi: http://doi.org/10.15587/2519-4852.2018.140756
- Poriadok provedennia naukovymy ustanovamy doslidiv, eksperymentiv na tvarynakh (2012). Nakaz Ministerstva osvity, nauky, molodi ta sportu Ukrainy. Nakaz No. 249. 01.03.2012. Ofitsiinyi visnyk Ukrainy, 24, 82.
- Rybolovlev, Iu. R., Sidliarov, D. P., Afonin, N. I. (1981). Prognosticheskaia otsenka bezopasnosti veschestv dlia cheloveka po konstantam ikh biologicheskoi aktivnosti. Toksikologicheskie aspekty bezopasnosti gotovykh lekarstvennykh form. Moscow, 9–10.
- Nasri, H., Rafieian-Kopaei, M. (2014). Metformin: Current knowledge. International Journal of Research in Medical Sciences, 19 (7), 658–664.
- Mauvais-Jarvis, F. (2018). Gender differences in glucose homeostasis and diabetes. Physiology & Behavior, 187, 20–23. doi: http://doi.org/10.1016/j.physbeh.2017.08.016
- Zand, A., Ibrahim, K., Patham, B. (2018). Prediabetes: Why Should We Care? Methodist DeBakey Cardiovascular Journal, 14 (4), 289–297. doi: http://doi.org/10.14797/mdcj-14-4-289
- Sakoda, H., Ogihara, T., Anai, M., Funaki, M., Inukai, K., Katagiri, H. et. al. (2000). Dexamethasone-induced insulin resistance in 3T3-L1 adipocytes is due to inhibition of glucose transport rather than insulin signal transduction. Diabetes, 49 (10), 1700–1708. doi: http://doi.org/10.2337/diabetes.49.10.1700
- Bardy, G., Virsolvy, A., Quignard, J. F., Ravier, M. A., Bertrand, G., Dalle, S. et. al. (2013). Quercetin induces insulin secretion by direct activation of L-type calcium channels in pancreatic beta cells. British Journal of Pharmacology, 169 (5), 1102–1113. doi: http://doi.org/10.1111/bph.12194
- Eitah, H. E., Maklad, Y. A., Abdelkader, N. F., Gamal el Din, A. A., Badawi, M. A., Kenawy, S. A. (2019). Modulating impacts of quercetin/sitagliptin combination on streptozotocin-induced diabetes mellitus in rats. Toxicology and Applied Pharmacology, 365, 30–40. doi: http://doi.org/10.1016/j.taap.2018.12.011
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