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Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
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Quercetin/beta-cyclodextrin solid complexes prepared in aqueous solution followed by spray-drying or by physical

Greice S Borghetti1, Ivana S Lula, Ruben D Sinisterra

  • 1Universidade Federal do Rio Grande do Sul, Porto Alegre, Rio Grande do Sul, Brazil.

AAPS Pharmscitech
|March 13, 2009
PubMed
Summary

Optimizing operating conditions improved quercetin solubility with beta-cyclodextrin. Spray-drying yielded a solid complex, but physical mixtures offered comparable solubility enhancement for quercetin complexation.

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science

Background:

  • Quercetin, a flavonoid, exhibits poor aqueous solubility, limiting its bioavailability.
  • Beta-cyclodextrin (β-CD) is a cyclic oligosaccharide used to enhance the solubility and stability of poorly soluble drugs.

Purpose of the Study:

  • To investigate the impact of operating conditions on quercetin-β-CD complexation.
  • To determine the optimal conditions for quercetin solubility enhancement.
  • To compare different methods of preparing quercetin-β-CD inclusion complexes.

Main Methods:

  • A 2(3) factorial design was employed to study temperature, stirring time, and quercetin excess.
  • Phase-solubility diagrams were used to determine stoichiometry and stability constants.
  • Semi-industrial production involved aqueous complexation followed by spray-drying.
  • Physical mixtures were prepared and characterized using spectroscopic and thermal analyses.

Main Results:

  • Optimal conditions for highest aqueous solubility were 37°C, 24h, and 6 mM quercetin.
  • The quercetin/β-CD complex exhibited a 1:1 stoichiometry and a stability constant (Ks) of 230 M⁻¹.
  • Spray-drying yielded a complex with adequate yield (77%) but low quercetin concentration and complexation efficiency.
  • The solubility enhancement via spray-drying was 4.6-fold (15 mM β-CD), while physical mixtures showed a 2.2-fold enhancement.

Conclusions:

  • Operating conditions significantly influence quercetin complexation with β-CD.
  • Spray-drying is a viable method for producing quercetin-β-CD complexes, though optimization is needed for higher drug loading.
  • Physical mixture preparation offers a simpler alternative with comparable solubility enhancement to pre-spray-drying aqueous solutions.