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Exploring Taxifolin Polymorphs: Insights on Hydrate and Anhydrous Forms.

Fernanda Cristina Stenger Moura1, Nicola Pinna2, Riccardo Vivani2

  • 1Programa de Pós Graduação em Ciências-PPGCF, Universidade do Vale do Itajaí, Itajaí 88302-202, SC, Brazil.

Pharmaceutics
|September 28, 2021
PubMed
Summary

Researchers identified six crystalline phases of taxifolin (dihydroquercetin), including hydrated and anhydrous forms. These polymorphs exhibit high stability, with potential applications suggested by their solubility characteristics.

Keywords:
X-ray powder diffractiondifferential scanning calorimetryequilibrium solubilityintrinsic solubilitypolymorphismtaxifolinthermogravimetry

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Area of Science:

  • Pharmacology
  • Materials Science
  • Crystallography

Background:

  • Taxifolin (dihydroquercetin) exhibits significant biological properties.
  • Understanding its solid-state forms is crucial for formulation and application.

Purpose of the Study:

  • To identify and characterize different crystalline polymorphs of taxifolin.
  • To investigate the stability and solubility of these taxifolin forms.

Main Methods:

  • Crystallization in various solvents.
  • X-ray powder diffraction (XRPD) for phase identification.
  • Differential scanning calorimetry (DSC) and thermogravimetry (TGA) for thermal analysis.
  • Scanning electron microscopy (SEM) and hot stage microscopy (HSM) for morphological characterization.
  • Solubility and dissolution rate studies.

Main Results:

  • Six distinct crystalline phases of taxifolin were identified: one fully hydrated, one partially hydrated, one monohydrated, two anhydrous polymorphs, and one likely solvated phase.
  • Unit cell parameters were determined for three phases, and one anhydrous polymorph was structurally characterized by XRPD.
  • Both hydrate and anhydrous forms demonstrated high stability under harsh storage conditions.
  • The anhydrous form converted to the hydrate form during solubility studies.
  • Taxifolin equilibrium solubility was determined to be approximately 1.2 mg/mL.
  • The intrinsic dissolution rate of hydrate taxifolin was 56.4 μg cm⁻² min⁻¹.

Conclusions:

  • Taxifolin can exist in multiple crystalline forms, including hydrated and anhydrous polymorphs.
  • The identified taxifolin polymorphs possess remarkable stability.
  • The solubility and dissolution characteristics suggest potential for various applications, warranting further investigation.