Pre-clinical screening of permeation enhancers for oral peptide administration in oral dosage forms: update on GI-ORIS

Despite decades of intensive research, oral delivery of macromolecules remains a largely unresolved challenge. Advancements in the field of peptide therapeutics, resulting in highly potent and stabilized compounds, closes an important gap in the field and provides renewed hope towards having these drugs in an oral form. However, the ability to create an optimal delivery system that ensures sufficient oral bioavailability remains key. This presentation will cover the current limitations in oral peptide delivery and progress in the field. Emphasis will be given to high throughput-based excipient screening approaches to increase gastrointestinal absorption of macromolecules such as peptides. Furthermore, key learnings translating liquid drug delivery systems to clinically viable solid dosage formulations will be covered through case studies. How well different pharmacokinetic in vivo models correlate and what ultimately provides the greatest prediction to humans, remain elusive. To that end, this presentation will also discuss certain aspects how species related intestinal absorption can be investigated to ensure large animal to human translatability.