Enabling Oral Delivery of Peptides through Molecular and Formulation Design

The oral delivery of peptides faces several significant challenges due to their inherent instability, limited permeability, and vulnerability to enzymatic degradation in the gastrointestinal tract. Compounding these issues is the negative food effect, which necessitates dosing in a fasted state, complicating patient compliance. To overcome these obstacles, a multifaceted approach is essential, focusing on innovations in both molecular and formulation design.

Molecular design strategies can enhance the stability of peptides in the gastrointestinal environment. In addition, generating fundamental understanding how peptides interact with bile salts, which may contribute to the negative food effect, could help develop better peptide molecules. Alongside these molecular innovations, advancements in formulation techniques are also essential to ensure that peptides achieve adequate exposure for clinical effectiveness. The application of absorption enhancers, a technology often reported in the literature, is one viable solution for improving peptide bioavailability. The current presentation shares J&J approach to enable oral delivery of peptides via molecular and formulation design.