A Robust And Scalable Strategy To Develop Monodisperse Nanosuspension Formulation For A Poorly Soluble Drug Substance

One of the most significant challenges in drug discovery and development is the low aqueous solubility of many compounds, which often leads to poor bioavailability and limits their progression into preclinical and clinical studies. Among the various strategies used to overcome this hurdle, nanosizing has emerged as one of the most effective approaches to enhance solubility and enable compounds to advance into toxicity and pharmacokinetic studies. Nanosuspensions offer distinct advantages, including broad applicability across different compound classes, lower excipient or vehicle requirements, and ease of administration.

Nanosuspensions are colloidal dispersions composed of drug particles uniformly distributed in an aqueous medium containing carefully selected wetting agents and stabilizers. These formulations typically have particle sizes below 1 µm—ideally under 0.5 µm—which significantly increases the surface area and promotes faster dissolution. Achieving this submicron particle size requires precise optimization of formulation components and ball milling process parameters.

This case study highlights how Aragen’s formulation scientists successfully designed a robust and scalable nanosuspension formulation for a poorly soluble drug substance. By tailoring the formulation strategy, selecting the appropriate excipients, and fine-tuning process conditions, the team was able to improve the compound’s bioavailability and in vivo exposure, enabling further development.