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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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Effect of Basic Amino Acids on Folic Acid Solubility
Karen Pérez-Carreón1, Luz María Martínez1, Marcelo Videa1
1School of Engineering and Sciences, Tecnologico de Monterrey, Campus Monterrey, Ave. Eugenio Garza Sada 2501 Sur. Monterrey N.L., Monterrey 64849, Mexico.
Pharmaceutics
|November 25, 2023
Summary
Folic acid (FA) solubility was significantly enhanced by forming binary formulations with basic amino acids (arginine and lysine). This co-amorphization strategy offers a promising approach for improving FA bioavailability in pharmaceutical applications.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Biochemistry
Background:
- Folic acid (FA) is crucial for preventing neural tube defects but suffers from poor solubility (Class IV BCS drug).
- Enhancing FA solubility is essential for effective pharmaceutical formulations.
- Amino acids (AA) can improve the solubility of poorly soluble drugs through co-amorphization or salt formation.
Purpose of the Study:
- To investigate the effect of basic amino acids (arginine and lysine) on folic acid solubility.
- To determine the optimal molar ratio for FA-AA binary formulations.
- To characterize the physical and chemical properties of the resulting formulations.
Main Methods:
- Conductimetric titration was used to determine the effective molar ratio for maximizing FA solubility.
- Binary formulations of FA with arginine and lysine were prepared using various methods.
- Characterization included differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD) to confirm amorphous systems.
Main Results:
- A 1:2.5 FA:AA molar ratio was found to maximize solubility for both arginine and lysine.
- The binary formulations exhibited significantly enhanced solubility, increasing 5500-6000 times compared to pure FA.
- Preparation methods influenced the morphological properties of the amorphous binary systems.
Conclusions:
- Co-amorphization with basic amino acids (arginine and lysine) effectively enhances folic acid solubility.
- The developed FA-AA binary systems represent a promising strategy for improving FA bioavailability.
- Understanding morphological properties is key for potential pharmaceutical scale-up.
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