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Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid
Published on: September 20, 2017
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Genistein Co-Amorphous Systems with Amino Acids: An Investigation into Enhanced Solubility and Biological Activity
Ewa Garbiec1, Natalia Rosiak1, Przemysław Zalewski1
1Department of Pharmacognosy and Biomaterials, Poznan University of Medical Sciences, 3 Rokietnicka St., 60-806 Poznan, Poland.
Pharmaceutics
|December 23, 2023
Summary
Genistein
Area of Science:
- Pharmacology
- Biochemistry
- Materials Science
Background:
- Genistein, an isoflavone, exhibits antioxidant and antidiabetic properties but is limited by poor solubility.
- Low solubility hinders the bioavailability and therapeutic efficacy of genistein.
- Developing strategies to enhance genistein's solubility is crucial for its pharmaceutical applications.
Purpose of the Study:
- To enhance the solubility and biological activity of genistein using co-amorphous systems.
- To investigate the potential of amino acids, selected via computational methods, in forming genistein co-amorphous systems.
- To evaluate the physicochemical properties, stability, and biological performance of the developed genistein co-amorphous systems.
Main Methods:
- Co-amorphous systems of genistein with lysine and arginine were synthesized.
- Amorphous state confirmed by X-ray powder diffraction (XRPD).
- Characterization using thermo-gravimetry (TGA), differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR), and scanning electron microscopy (SEM).
- Physical stability assessed over 6 months.
- Apparent solubility determined in aqueous media.
- In vitro gastrointestinal permeability evaluated using the parallel artificial membrane permeability assay (PAMPA).
- Antioxidant activity assessed via DPPH and CUPRAC assays.
- Alpha-glucosidase inhibition measured.
- Glass transition temperatures (Tg) determined by DSC.
Main Results:
- Co-amorphous systems with lysine and arginine were successfully synthesized and confirmed to be amorphous.
- The lysine-containing system showed the most significant improvement in apparent solubility and antioxidant activity.
- Both co-amorphous systems exhibited enhanced α-glucosidase inhibition compared to acarbose.
- Systems maintained physical stability throughout the 6-month storage period.
- DSC and FTIR analyses confirmed system homogeneity and molecular interactions.
Conclusions:
- Co-amorphous systems incorporating lysine and arginine effectively enhance genistein's solubility and biological properties.
- The lysine-based system demonstrates superior performance in solubility enhancement and antioxidant activity.
- These co-amorphous systems hold significant potential for improving genistein's therapeutic efficacy, particularly for type 2 diabetes management.
- Further development of these systems could lead to improved drug delivery and patient outcomes.
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