In-situ Eutectic Formation during Reactive Melt Extrusion as a Mean to Improve Dissolution Performance for Benzimidazole Derivative Drugs

Benzimidazole is widely regarded as an important pharmacophore within the field of cancer research owing to its versatile scaffold that could be derivatised to provide a range of mechanisms of action against tumour progression. Facile synthetic strategies based on the bicyclic fused ring have led to potential and ongoing developments of target-specific and highly-effective anticancer agents. Such a promising central structure, however, inherits poor aqueous solubility from one of the parent reagents, benzene, limiting the derivatives’ therapeutic effectiveness and stalling their development progress. In the current study, we explored the potential of forming a eutectic complex between a benzimidazole derivative drug, albendazole (ABZ), and a highly soluble guest molecule, maleic acid (MA), as a solubility enhancement strategy. The said eutectic system was formed in-situ within polymeric formulation matrices during hot-melt extrusion (HME) processing.