This presentation will run through a range of solid form strategies for increasing oral bioavailability and their relative advantages and disadvantages, including salt formation, co-crystallization, spray drying of amorphous solid dispersions, and Controlled Expansion of Supercritical Solutions (CESS®). The dissolution behavior of nanoparticles created using different techniques will be explored, along with the importance of crystallinity in the context of drug design.
To this end, the presentation will feature case study examples, including piroxicam (PRX), fenofibrate (FEN) and budesonide (BUD), demonstrating methods for controlling crystallinity, particle size and polymorphism using supercritical carbon dioxide to achieve the desired particle attributes.
A closer look will be taken at how the use of nanoparticles can contribute to patient comfort and quality of life, examining how reducing particle size can lead to, for example, increased drug loading and lower pill burden. Finally, the presentation will also explore how sparse-data AI can be used to predict both a drug candidate’s propensity to crystallize and its amenability for a specific nanoparticle engineering technique, highlighting that through this technology it is possible to determine that 87% of all API molecules whose structure has been publicly disclosed are amenable to CESS®. Taken together, the presentation will serve to spotlight the game-changing nature of patient-centric nanoparticle drug discovery and design powered by sparse-data AI.