Improved solubility of hydrophobic drugs using hot melt extrusion technology

Abstract

It is estimated that about 40% of all new chemical entities have poor bioavailability because of low aqueous solubility. This percentage still increases due to combinatorial chemistry and the impact of lipophilic receptors1. Solubility is essential for the therapeutic effectiveness of the drug, independent of the route of administration. Poorly soluble drugs are often a challenging task for formulators in the industry. Conventional approaches for enhancement of solubility have limited applicability, especially when the drugs are poorly soluble simultaneously in aqueous and in non-aqueous media. Solubilisation may be affected by co-solvent water interaction, micellar solubilisation, reduction in particle size, inclusion complexes, solid dispersion, and change in polymorph