Effect of stoichiometry upon the characteristics of quercetin-arginine cocrystals formulated through solution crystallization

OBJECTIVE: The aim of this study is to demonstrate the effect of stoichiometry upon characteristics of quercetin-arginine (QCT-Arg) cocrystals.

SIGNIFICANCE: Quercetin (QCT) is a most abundant flavonoid in vegetables and fruits and has been widely used as an antioxidant. However, its oral bioavailability remains low due to poor aqueous solubility. We illustrate that QCT-Arg cocrystals formulated through an optimized stoichiometry can be a useful approach for its solubilization.

METHOD: Cocrystals were prepared using solvent evaporation method. Characterizations were performed through microscopic, spectroscopic, and thermal techniques. The stoichiometry was confirmed from the binary phase diagram which was prepared using thermograms derived from differential scanning calorimetric experiments.

RESULT: Cocrystal formation was accompanied by the conversion of isotropic phase into anisotropic one. Thread-like cocrystals were formed, regardless of QCT-Arg stoichiometry and solvent's polarity. Spectral analyses suggested that cocrystal structure was held together by hydrogen bonding between QCT and Arg. We ruled out the existence of eutectic mixture based on the observation of two eutectic points in the binary phase diagram.

CONCLUSION: Morphology of cocrystals remained unaffected by the solvent type, stoichiometry and the presence of surfactant. We noticed that the cocrystals could improve the aqueous solubility of QCT.

Medienart:

E-Artikel

Erscheinungsjahr:

2024

Erschienen:

2024

Enthalten in:

Zur Gesamtaufnahme - volume:50

Enthalten in:

Drug development and industrial pharmacy - 50(2024), 2 vom: 20. Feb., Seite 163-172

Sprache:

Englisch

Beteiligte Personen:

Mishra, Mahima [VerfasserIn]
Agrawal, Shivanshu [VerfasserIn]
Bahadur, Pratap [VerfasserIn]
Tiwari, Sanjay [VerfasserIn]

Links:

Volltext

Themen:

9IKM0I5T1E
Antioxidants
Binary phase diagram
Flavonoids
Hydrogen bonding, solvent evaporation, coformer
Journal Article
Quercetin
Solvents
Spectral analysis, thermogram

Anmerkungen:

Date Completed 23.02.2024

Date Revised 23.02.2024

published: Print-Electronic

Citation Status MEDLINE

doi:

10.1080/03639045.2024.2306281

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM36717524X