Improve Solubilization Kinetics of Poorly Soluble Drugs (BCS Class II/IV)

NCE under development. Low, pH dependent solubility. Poorly soluble molecule (<10 μg/ml) at intestinal pH. Low-medium permeability. Medium to high dosing required.
Drug molecule has poor bioavailability caused by low solubility and precipitation in intestinal fluids.

Applying Variosol technology it was possible to:

  • formulate the drug as solid dispersion into amphyphilic, lipid-based microspheres, and improve its dissolution rate into intestinal fluids
  • develop a solid micronized system with self-emulsifying properties, with drug loading up to 40% w/w
  • improve bioavailability (more than doubled AUC vs. formulated drug solution) after oral administration in beagle dogs (PK data not shown)

BCS Class II drug dissolution profile in fed simulated small intestinal fluid (FeSSIF), sink conditions. Microparticles formulations based on Variosol show a fast and almost complete drug dissolution vs. drug in aqueous suspension.

BCS Class II drug solubilization kinetics in oversaturated conditions (FeSSIF). Microparticles formulations based on Variosol show a high capability to maintain drug in solution in supersaturated conditions, facilitating drug absorption from the intestinal tract.