Spray-Dry Process Application in the Pre-Clinical Stage of Drug Development

• Amorphous Solid Dispersions (ASD)
  • Background Concepts and Approaches
  • Feasibility in early Stage of Drug Development
• Spray Dry Dispersion (SDD)
  • Optimization of Formulation and Process Parameters for Pre-clinical Formulation Support

In oral drug delivery, Amorphous Solid Dispersion (ASD) have become an established approach to enhance aqueous dissolution, improve in-vivo absorption and bioavailability of poorly soluble molecules. Among various methods to produce ASD formulations, spray drying represents one of the most well established manufacturing techniques. However, this technology in early stage of drug development often faces different challenges, from limited API availability to numerous formulation and process variables, which can affect the range of possible screenings, increasing the development timeline and the resources requirements.

This research presentation introduces the development of a reproducible and efficient spray-drying platform to address the aforementioned challenges. The implemented strategy consisted in identifying optimized pre-set spray dry parameters to enable ASDs early screening and feasibility, excluding the need of individual optimization. Using a BUCHI mini spray-dryer B-290, the impact of two key  variables of spray drying (solid load and atomization pressure) was evaluated on the critical quality attributes (CQAs) of the ASDs, including yields, particle sizes, and in vitro release profile.  Additional variables, such as polymers, drugs type and drug loadings were also taken into consideration to confirm the pre-defined parameters. Furthermore, the strategy was applied from small to large-scale batches to support various toxicology studies.

Marika Nespi, Senior Principal Scientific Researcher , Genentech