Fluidized Bed Hot-Melt Granulation as a Tool to Improve Curcuminoid Solubility

Area of Science:

• Pharmaceutical Technology
• Materials Science
• Natural Products Chemistry

Background:

• Curcumin, a key compound from Curcuma longa L., shows therapeutic potential but suffers from poor solubility and bioavailability.
• Existing strategies to enhance curcumin's solubility have limitations.
• Hydrophilic material-based granulation for curcumin has not been previously explored.

Purpose of the Study:

• To develop curcumin granules using fluidized bed hot-melt granulation with the hydrophilic carrier Gelucire® 50:13.
• To investigate the impact of Gelucire® 50:13 and lactose content on granule properties.
• To evaluate the enhanced solubility, dissolution, and stability of the developed curcumin granules.

Main Methods:

• Fluidized bed hot-melt granulation utilizing Gelucire® 50:13 as a hydrophilic carrier.
• Factorial design to optimize granule formulation (Gelucire® 50:13 and lactose content).
• Characterization included physical properties, thermal analysis (DSC, TGA), solid-state analysis (XRD, FTIR), solubility, and dissolution testing.

Main Results:

• The optimized formulation achieved a remarkable 4642-fold increase in curcumin solubility compared to a physical mixture.
• Dissolution tests demonstrated significantly improved drug release: up to 70% at pH 1.2 and 80% at pH 5.8/7.4 within 45 minutes.
• Granules exhibited good stability over a 9-month period, with enhanced solubility and dissolution profiles maintained.

Conclusions:

• Fluidized bed hot-melt granulation with hydrophilic binders is a promising technique for producing curcumin solid forms.
• This method effectively overcomes curcumin's low solubility and enhances its oral bioavailability.
• The developed granules offer a stable and effective alternative for curcumin drug delivery.