Improving solubility remains one of the greatest barriers to successful drug delivery. Biotech and pharma development teams are constantly under pressure to rapidly advance molecules to the next development milestone and get to market as quickly as possible. However, progress is often constrained by formulation challenges in early stage drug development, with the prevalence of poorly soluble compounds within the development pipeline, being a prime example.
Pharmaceutical formulation scientists have an increasing range of strategies and technologies available to support successful solubility enhancement. These include amorphous forms, particle size reduction and lipid-based drug delivery systems.
However, such technologies cannot be successful in isolation. Moving a molecule quickly towards application as a medicine requires a strategy underpinned by a fundamental understanding of the compound itself, and critically a formulation strategy that does not rely solely on potentially misleading nonclinical data. The ability to screen a range of technologies and dosage forms using biorelevant in vitro screening tools and physiologically based in-silico models to flag developability problems is essential before quickly transitioning drug candidates into human PK studies to understand a molecules full potential for success.
This presentation uses expert insight and case studies to explore formulation and solubility challenges and discuss the best strategies and technologies for advancing poorly soluble molecules, to deliver success.
Key Learning Objectives
- Pharmaceutics and biopharmaceutics profiling of NCEs
- The DCS classification system as a foundation for creating a formulation development roadmap
- Formulation strategies for DCS Class IIa and IIb compounds
- A review of the formulation technologies available from size-reduction, to lipid systems and amorphous forms
- Selecting appropriate biorelevant in vitro characterization methods to inform potential clinical performance
- The application and benefits of PBPK modelling to predict clinical exposure
- Choosing the right formulation for preclinical studies and dosage forms for First-in-Human (FIH) studies