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Preparation of Naringenin Solution for In Vivo Application
Published on: August 10, 2021
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Naringenin Cocrystals Prepared by Solution Crystallization Method for Improving Bioavailability and
Wenxia Cui1, Zehui He1, Yongtai Zhang1
1Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, China.
AAPS Pharmscitech
|February 17, 2019
Summary
Cocrystal formation significantly enhances naringenin
Area of Science:
- Pharmacology and Pharmaceutical Sciences
- Materials Science
- Biochemistry
Background:
- Naringenin possesses anti-inflammatory, hypolipidemic, and hepatoprotective properties.
- Poor water solubility limits naringenin's oral bioavailability and therapeutic efficacy.
- Cocrystal formation is explored as a strategy to overcome these limitations.
Purpose of the Study:
- To develop and characterize naringenin cocrystals with improved solubility and oral bioavailability.
- To evaluate the in vivo pharmacokinetic and pharmacodynamic effects of naringenin cocrystals.
- To assess the potential of naringenin cocrystals in treating hyperlipidemia.
Main Methods:
- Cocrystals were prepared using the solution crystallization method with various coformers (nicotinamide, isonicotinamide, caffeine, betaine, L-proline).
- Cocrystal formation was confirmed using differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier-transform infrared (FT-IR) spectroscopy.
- Stoichiometric ratios were determined by nuclear magnetic resonance (NMR) spectroscopy.
- In vivo studies involved oral administration to rats and mice to assess bioavailability, pharmacokinetics, and anti-hyperlipidemic effects.
Main Results:
- Cocrystal formation markedly improved naringenin's solubility and dissolution rate.
- Naringenin-L-proline and naringenin-betaine cocrystals showed significantly higher oral bioavailability in rats compared to pure naringenin (p < 0.05).
- Specific increases in Cmax and AUC were observed for naringenin-L-proline (2.00-fold and 2.39-fold) and naringenin-betaine (3.35-fold and 4.91-fold).
- Naringenin-betaine cocrystals enhanced liver drug distribution and demonstrated improved anti-hyperlipidemic effects in a mouse model.
Conclusions:
- Cocrystal formation is an effective strategy to enhance the solubility and oral bioavailability of naringenin.
- Naringenin-betaine cocrystals show particular promise for improving naringenin's therapeutic potential in treating hyperlipidemia.
- This approach offers a viable route for developing naringenin-based therapies with improved pharmacokinetic profiles.
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