Formulation and Quality – Chemical
2019 PharmSci 360
Recent estimates suggest that as many as 75% of new chemical entities are poorly soluble compounds. Achieving sufficient bioavailability via the preferred oral delivery route with these types of molecules places a significant burden on effective formulation design. However, due to the time and expense of formulation optimization, sub-optimal fit-for-purpose formulations may hinder pre-clinical performance. Then, if progressed into clinical development, most fit-for-purpose formulations require modifications during scale-up that increase cost and time to market, at best, and can adversely affect in-vivo bioavailability, at worst. Here, we discuss hydrogels modified with hydrophobic domains (or “nano-templated hydrogels”) as a novel oral dosage form capable of overcoming current formulations challenges facing poorly soluble compounds. Nano-templated hydrogels simultaneously transform the molecule into nanocrystals and encapsulate them in a customizable, pre-formed semi-solid gel. Importantly, the solid state properties (e.g., polymorph, crystal size, and drug loading) are independent of scale, which can facilitate seamless clinical translation using the same commercially viable dosage form.