Ready-to-Use Solubilisation Platform for Challenging APIs

Poor aqueous solubility remains one of the most significant challenges in drug development, often limiting bioavailability and increasing formulation complexity. This prevalence extends formulation timelines, increases development costs, and often limits therapeutic efficacy despite promising pharmacological activity. For poorly soluble active pharmaceutical ingredients (APIs), inadequate dissolution translates directly into reduced oral bioavailability, variable pharmacokinetic profiles, and the need for higher doses to achieve therapeutic plasma concentrations. 

This study evaluated ready-to-use pre-emulsion concentrates containing carefully selected oils, surfactants, co-surfactants, and water as a universal solubilisation platform. The objective was to improve API solubility, simplify formulation development, and provide a scalable solution suitable for a broad range of active pharmaceutical ingredients across multiple BCS classes. IMCD developed and evaluated ready-to-use pre-emulsion (pre-mix) concentrates as a universal solubilisation platform to enhance the solubility, bioavailability, and formulation efficiency of poorly water-soluble APIs across multiple dosage forms. 

The platform was successfully evaluated with a diverse range of APIs, including upadacitinib hemihydrate, loratadine, famotidine, fenofibrate, paracetamol, lumefantrine, clotrimazole, budesonide, terbinafine HCl, fexofenadine HCl, and apremilast, highlighting its broad applicability across different chemical properties and BCS classes. 

Suitable for oral, topical, and nasal dosage forms, these ready-to-use pre-emulsion concentrates offer formulators a scalable and efficient solution that can reduce development time, enable high drug loading, and accelerate the path from API selection to finished drug product.