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Crystallization of Membrane Proteins in Lipidic Mesophases
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Chrysin cocrystals: Characterization and evaluation.

Renu Chadha1, Yashika Bhalla1, Avdesh Nandan1

  • 1University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India.

Journal of Pharmaceutical and Biomedical Analysis
|November 30, 2016
PubMed
Summary
This summary is machine-generated.

This study developed new chrysin cocrystals using a solvent-free method to improve its bioavailability. The novel cocrystals demonstrated significantly enhanced solubility and therapeutic effects.

Keywords:
Anti-inflammatoryAntihaemolyticAntioxidantChrysinCocrystalsDSCFTIRPXRDPharmacokinetics

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Area of Science:

  • Pharmacology
  • Materials Science
  • Supramolecular Chemistry

Background:

  • Chrysin, a flavone, exhibits beneficial effects but suffers from poor bioavailability due to low aqueous solubility.
  • Low solubility and absorption limit the therapeutic potential of chrysin in pharmaceutical applications.

Purpose of the Study:

  • To enhance the solubility and bioavailability of chrysin.
  • To synthesize novel chrysin cocrystals using a solvent-free mechanochemical approach.
  • To investigate the supramolecular interactions and physicochemical properties of the new cocrystals.

Main Methods:

  • Solvent-free mechanochemical synthesis of chrysin cocrystals with cytosine and thiamine hydrochloride.
  • Characterization using Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FT-IR), Solid State Nuclear Magnetic Resonance (SSNMR), and Powder X-Ray Diffraction (PXRD).
  • Evaluation of solubility, dissolution profiles, and in vitro/in vivo biological activities.

Main Results:

  • Successful synthesis of chrysin cocrystals with cytosine and thiamine hydrochloride.
  • Cocrystals exhibited a common supramolecular motif (OH⋯Narom interaction) involving hydrogen bonding.
  • Significant 3-4 fold increase in solubility and dissolution rate observed for the cocrystals.
  • Improved in vitro and in vivo antioxidant, antihaemolytic, and anti-inflammatory activities.

Conclusions:

  • Mechanochemical synthesis offers a viable route for developing chrysin cocrystals with improved physicochemical and biological properties.
  • Enhanced solubility and bioavailability of chrysin cocrystals can lead to better therapeutic outcomes.
  • This approach provides a new strategy for optimizing the delivery of phytonutrients.