DRUG PRODUCT DESIGN FOR DELIVERY OF CHALLENGING MOLECULES

The landscape for oral drug delivery is rapidly evolving as the molecules to be delivered become increasingly more complex. The time when the rule of five governed the perspective on effective oral delivery has long passed, and we are regularly tasked with developing oral products for low solubility and low permeability small molecules, PROTACs, peptides and other challenging moieties. While technology selection for bioavailability enhancing enabled formulations often emphasizes design and development of an enabled intermediate, the increasing complexity of the molecular landscape necessitates a more comprehensive approach that considers the drug product design and manufacturability simultaneously with intermediate development. This is especially relevant as clinical development timelines compress and advanceable and robust formulations are needed right from the start of development.

In this talk we illustrate several case studies demonstrating how a fundamental understanding of molecular properties combined with a strategic vision for drug product design can lead to effective and advanceable formulations for even the most challenging drug products. Among the examples highlighted are development of enabled tablet formulations designed as an alternative to amorphous dispersions, product design for amorphous dispersions when alternative technologies fail to provide sufficient enablement, and considerations on the product and process design for oral solid dosage forms containing permeation enhancers.

Key Takeaways

The "rule of five" (ByRo5) is no longer sufficient as drug developers frequently encounter molecules with low solubility and permeability, driving them toward new and innovative formulation strategies
A strategic vision for drug product design combined with an understanding of molecular properties can lead to successful formulation development, even for challenging compounds
Formulation development should not solely focus on enabling intermediates. Product design and manufacturability must be considered in conjunction with intermediate development.

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Yizheng Cao

Principal Scientist, Process and Product Development

Yizheng Cao is a Principal Scientist in the Process and Product Development department at Serán. He leads a team of scientists and engineers in investigating new drug substances and identifying shortcomings for oral bioavailability. He and his team then screen and select drug product intermediates that address those issues, and develop drug product formulations. During his time at Serán, his research has focused on understanding how polymers, excipients, and physiological factors influence speciation, bioavailability, and absorption of drug substances and amorphous solid dispersions.

Prior to Serán, Yizheng worked in a large CDMO for about 7 years, primarily focusing on pre-formulation of drug substances.

Yizheng holds an undergraduate degree in Physics from Nanjing University and a Ph.D. in Materials Science and Engineering from Purdue University.

About Serán

Serán's Science-First Approach

Serán Bioscience is a science-based CDMO that specializes in a variety of drug delivery and formulation approaches suited to optimizing bioavailability. Our experienced formulation team will work with you to identify an appropriate technology and formulation strategy to meet your program’s unique needs. We take a comprehensive approach to formulation design that considers the physiochemical properties of the API, the target product profile, and your program’s objectives and constraints to develop scalable formulations using efficient and material-sparing approaches.

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