Enhanced dissolution rate of nimodipine through β-lactoglobulin based formulation

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Amorphous solid dispersions (ASDs) are crucial for improving the solubility and dissolution rates of poorly water-soluble drugs.
• The choice of carrier significantly impacts the properties, stability, and performance of ASDs.

Purpose of the Study:

• To investigate the solid-state properties, physical stability, and in vitro dissolution of nimodipine ASDs.
• To compare the efficacy of a novel carrier, β-lactoglobulin (BLG), against a traditional carrier, polyvinylpyrrolidone (PVP).

Main Methods:

• ASD formulations of nimodipine with PVP and BLG were prepared using ball milling at various drug loadings (10–40%).
• Solid-state characterization was performed using X-ray powder diffraction.
• Physical stability was assessed under accelerated storage conditions (40°C/75% RH).
• In vitro dissolution studies were conducted in simulated gastric and intestinal fluids.

Main Results:

• All formulations were initially amorphous, but only ASDs with BLG at 10% and 17.5% drug loading remained amorphous after storage.
• PVP-based ASDs and BLG-based ASDs at ≥25% drug loading showed limited drug release.
• BLG-based ASDs at 10% and 17.5% drug loading exhibited significantly enhanced drug release, with the 17.5% formulation achieving the highest Cmax.

Conclusions:

• The selection of carrier type and drug loading is critical for designing stable ASDs with enhanced dissolution.
• β-lactoglobulin shows promise as a carrier for improving the dissolution of poorly water-soluble drugs like nimodipine.
• Optimized BLG-based ASDs can achieve superior drug release profiles compared to traditional carriers.