The 9th International Mediterranean Symposium on Medicinal and Aromatic Plants (MESMAP-9), Ankara, Türkiye, 3 - 05 Mayıs 2023, ss.179-188
Quercetin is in the class of flavanols that its chemical formula is 3.3', 4', 5,7-pentahydroxyflavone. It has been demonstrated to possess diverse pharmacological benefits, such as serving as an antioxidant, having antiviral properties, and exhibiting anti-cancer effects. Quercetin has also anti-inflammatory and antinociceptive/analgesic properties. However, the low solubility and bioavailability of quercetin adversely affect its effectiveness. Thus, in order to increase the bioavailability and solubility of quercetin, it is aimed to examine the change in the analgesic effect of quercetin by preparing a biologically compatible cyclodextrin formulation that can be targeted to the tissues in this study. Quercetin and quercetin-β-cyclodextrin (β-CD) complex were administered intraperitoneally at doses of 3, 5, 10, and 20 mg/kg in mice. Time-dependent analgesic effects of pure quercetin and quercetin-β-CD were compared in hot-plate and tail-immersion tests, acute pain models tested supraspinal and spinal organization of pain respectively. Quercetin at the doses of 5, 10 and 20 mg/kg was found to increase pain thresholds against to thermal stimuli in tail immersion and hot plate tests in 30-180 min. time interval. Only the effect of 20 mg/kg quercetin weakened at 180 min. The effect at 3 mg/kg was observed only in hot-plate test at 120 min. β-CD complex prepared with 3 mg/kg quercetin showed significant analgesic effect in 30-180 min time intervals in both two tests. Additionally, the analgesic effect of the β-CD complex prepared with 20 mg/kg quercetin was not weakened in both tests like pure 20 mg/kg quercetin at 180 minutes. Thereby, it can be concluded that application of quercetin in β-CD complex is provided to improve pharmacokinetic properties such as bioavailability of quercetin. Thus, the efficacy and duration of action of quercetin were enhanced. This study displays the analgesic potential of quercetin by spinal and supraspinal regulations and the advantages of application in β-CD formulation for pain relief.