Formulation Development Strategy For Early Phase Human Studies

By Jim Huang, PhD, Founder & CEO, Ascendia Pharmaceuticals

Successful translation of discovery compounds into first-in-human (P1) and first-inpatient (P2) is one of the key challenges facing the pharmaceutical industry. To achieve these goals, a rational formulation development strategy will be critical to avoid costly drug development failures, while speeding up the development timeline in a cost-effective manner. This is particularly true for compounds with challenging properties in solubility and
bioavailability.

At the early phase of drug development, there is a limited supply of API available. Determination of an appropriate bioavailable formulation for animal PK, GLP toxicity, and first-in-human and first-in-patient is a challenging task. For poorly soluble and bioavailable compounds, development of formulations is usually achieved using drug delivery systems. Those development studies may involve the pre-formulation evaluation of the compound physicochemical biopharmaceutical properties, such as solubility and stability, in commonly used solvents and bio-relevant media, and permeability, etc. Afterward, optimization of solubility and bioavailability can be achieved by utilizing suitable delivery systems by screening a set of technology platforms, such as Ascendia’s AmorSol®, NanoSol®, and EmulSol®, that address different compound challenges in hydrophilicity, lipophilicity, and melting point.