<p>The reduced bioavailability of quercetin due to poor water solubility limits its therapeutic potential when taken orally. A technology for creating 1:1 complexes with β-cyclodextrin was proposed to mitigate these limitations. A linear dependence of the ligand concentration on the content of the complexing agent and a nine-fold increase in the solubility of the active substance were found during a preliminary assessment of the phase solubility of quercetin and β-cyclodextrin in an aqueous solution. A comparative analysis of the methods for obtaining the inclusion complexes found the highest efficiency for the grinding method (yield 96%) as compared with the mechanical mixing method (95%) and suspension followed by lyophilic drying (82%). A change in the structural characteristics of the complexes (disappearance of the absorption band of the carbonyl group at 1640 cm<sup>–1</sup> in the IR spectrum) indicated the possible partial incorporation of quercetin molecules in the internal cavity of β-cyclodextrin (correlation 0.61). At the same time, the composition obtained by the grinding method demonstrated greater efficiency of binding to the β-cyclodextrin molecule (correlation 0.61). All the complexes under consideration could increase the solubility of quercetin. Also, the best results were noted for inclusion complexes obtained by grinding, for which the solubility of the active substance was statistically significantly increased by 235 times as compared to the original substance.</p>

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Comparative Characteristics of Methods for Producing Quercetin Inclusion Complexes with β-Cyclodextrin to Increase Solubility

  • A. A. Danilova,
  • K. A. Gusev,
  • E. V. Vishnyakov,
  • D. N. Maimistov,
  • E. V. Flisyuk

摘要

The reduced bioavailability of quercetin due to poor water solubility limits its therapeutic potential when taken orally. A technology for creating 1:1 complexes with β-cyclodextrin was proposed to mitigate these limitations. A linear dependence of the ligand concentration on the content of the complexing agent and a nine-fold increase in the solubility of the active substance were found during a preliminary assessment of the phase solubility of quercetin and β-cyclodextrin in an aqueous solution. A comparative analysis of the methods for obtaining the inclusion complexes found the highest efficiency for the grinding method (yield 96%) as compared with the mechanical mixing method (95%) and suspension followed by lyophilic drying (82%). A change in the structural characteristics of the complexes (disappearance of the absorption band of the carbonyl group at 1640 cm–1 in the IR spectrum) indicated the possible partial incorporation of quercetin molecules in the internal cavity of β-cyclodextrin (correlation 0.61). At the same time, the composition obtained by the grinding method demonstrated greater efficiency of binding to the β-cyclodextrin molecule (correlation 0.61). All the complexes under consideration could increase the solubility of quercetin. Also, the best results were noted for inclusion complexes obtained by grinding, for which the solubility of the active substance was statistically significantly increased by 235 times as compared to the original substance.