This article investigates the complexation of astilbin (Ast), a poorly soluble flavonoid, with methyl-β-cyclodextrin (M-β-CD) to enhance its solubility, stability, and bioavailability. Astilbin exhibits many pharmacological activities such as selective immunosuppressive activity, anti-inflammatory and antioxidant activity, and hypoglycemic effect. Key findings:
- M-β-CD exhibited the strongest complexation ability with Ast compared to other β-CD derivatives. The complexation was characterized by UV spectroscopy, phase solubility, and NMR analysis.
- The Ast/M-β-CD complexes were prepared by co-grinding and found to significantly improve the dissolution and solubility of Ast (>43 mg/mL). M-β-CD also suppressed the crystallization of Ast, maintaining its supersaturated status.
- The Ast/M-β-CD complexes enhanced the stability of Ast in simulated gastrointestinal fluids and significantly improved its oral bioavailability in rats by 11.89 times compared to free Ast.
Wen-Xuan Zhang, Jian-Feng Zhou, Hai-Xia Xu, Wen-Jun Wang, Ji-Guang Chen, Qing-Feng Zhang (2025)
Enhanced solubility, stability, and bioavailability of astilbin via inclusion complexes formation with methyl-β-cyclodextrin. Colloids and Surfaces A: Physicochemical and Engineering Aspects 726, Part 3, 138088.
https://doi.org/10.1016/j.colsurfa.2025.138088