Skip to main content
CRS 2024 Annual Meeting and Exposition Main banner
Final Program


CRS Abstract Guide

Session: Plenary Duet III: Oral Delivery of Biologics: Challenges, Opportunities, and Clinical Successes

Plenary Duet III Oral Delivery of Biologics Challenges, Opportunities, and Clinical Successes

Thursday, July 11, 2024
12:00 PM - 1:30 PM CET
Location: Sala Europa
Oral Delivery of a PCSK9i Peptide - Preclinical & Clinical Investigations
This presentation will cover formulation development of a PCSK9i peptide for oral delivery. Several different absorption enhancer-based formulations were developed and assessed preclinically and the most promising formulations were selected for further evaluation in clinic. The presentation will touch upon how translation is from large animals to clinic and how certain permeation enhancers seem to underperform in clinic. 
Philip Jonas Sassene, PhD, Novo Nordisk A/S


From Farm to Pharmacy: A Strawberry-Derived Solution to Oral Protein Delivery
Oral delivery is the most patient-friendly mode of drug administration. Unfortunately, it is not possible for most protein and other macromolecular drugs because the gastrointestinal tract is not permeable to undigested large molecules. Although many chemical permeation enhancers have been identified that improve the intestinal absorption of biologics, they often cause cytotoxicity or damage the intestinal mucosa. To address this issue, we sought to identify a permeation enhancer derived from fruits and vegetables, hypothesizing that the compounds found in natural foods would be well-tolerated by the gastrointestinal tract. Following a screen of over 100 fruits, vegetables, herbs, and fungi, we identified strawberry as a potent enhancer of macromolecular permeability both in vitro and in vivo. Natural product chemistry techniques revealed pelargonidin, an anthocyanidin, as the active compound in strawberry. In mice, pelargonidin enabled 100% bioactivity of oral insulin relative to the current gold standard of subcutaneous injection, without causing toxicity following 30 days of daily treatment. These results underscore the potential of naturally derived compounds in biomedical applications and demonstrate pelargonidin as an especially potent new enhancer for the oral delivery of biologics.
Kathryn A. Whitehead, Carnegie Mellon University