Ethyl ferulate/β-cyclodextrin inclusion complex inhibits edema formation

Area of Science:

• Pharmacology
• Materials Science

Background:

• Ethyl ferulate, a rice hull derivative, exhibits antioxidant, anti-inflammatory, and neuroprotective properties.
• Low water solubility of ethyl ferulate limits its gastrointestinal absorption, bioavailability, and in vivo effect reproducibility.

Purpose of the Study:

• To enhance the solubility and bioavailability of ethyl ferulate.
• To develop stable inclusion complexes of ethyl ferulate with beta-cyclodextrin.
• To evaluate the anti-inflammatory activity of these complexes in vivo.

Main Methods:

• Inclusion complexes were prepared using physical mixing, malaxation, lyophilization, and spray drying.
• Characterization involved thermal analysis, X-ray diffraction (XRD), and Fourier-transform infrared spectroscopy (FTIR).
• Inclusion complex content, stability, dissolution, and anti-inflammatory efficacy (carrageenan-induced paw edema in rats) were assessed.

Main Results:

• Inclusion complexes demonstrated significantly increased solubility and stability compared to free ethyl ferulate.
• Malaxation, lyophilization, and spray-dried complexes exhibited superior inhibition of carrageenan-induced paw edema.
• The enhanced anti-inflammatory effect is attributed to improved solubility and dissolution profiles.

Conclusions:

• Stable inclusion complexes of ethyl ferulate with beta-cyclodextrin were successfully formed.
• These complexes possess potent anti-edematogenic activity, suggesting improved therapeutic potential.
• Complexation is a viable strategy to overcome ethyl ferulate's solubility limitations for enhanced bioavailability.