Enhanced Dissolution of Luteolin by Solid Dispersion Prepared by Different Methods: Physicochemical Characterization...

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Luteolin (LT) is a bioactive compound with poor oral bioavailability due to low solubility.
• Enhancing LT's solubility and dissolution is crucial for improving its therapeutic efficacy.

Purpose of the Study:

• To formulate and characterize luteolin solid dispersions (LT-SDs) using polyethylene glycol 4000 (PEG 4000).
• To enhance the dissolution rate and in vitro antioxidant activity of luteolin.
• To investigate the impact of different preparation methods (fusion, solvent evaporation, microwave irradiation) and mass ratios on LT-SD properties.

Main Methods:

• Formulation of LT-SDs using PEG 4000 at mass ratios of 1:1, 1:2, and 1:4.
• Preparation of SDs via fusion (FU), solvent evaporation (SE), and microwave irradiation (MI) methods.
• Characterization using DSC, XRD, SEM, IR, and NMR.
• Evaluation of in vitro dissolution and antioxidant activity.

Main Results:

• Solid-state characterization confirmed the formation of LT-SDs and the conversion of LT from crystalline to amorphous form.
• All prepared SDs showed significantly higher LT release compared to pure LT and physical mixture dispersions.
• The MI method at a 1:2 LT:PEG 4000 ratio exhibited maximum LT release (97.78%) and enhanced antioxidant activity.
• The SE method at a 1:4 ratio also showed high release (93.78%).

Conclusions:

• Solid dispersion technology using PEG 4000 is a promising strategy to overcome luteolin's poor solubility and bioavailability issues.
• The MI method is particularly effective for preparing LT-SDs with enhanced dissolution and therapeutic potential.
• Amorphous conversion and reduced particle size contribute to the improved performance of LT-SDs.