Development of permeability enhancers for oral peptide drug delivery

Macromolecular drug molecules demand advanced drug delivery systems to enable them to be developed as functioning medicines.

These drugs,  such as peptides,  have several advantages over traditional small-molecule drugs, including high potency, target specificity, and low toxicity, and they provide a diverse range of therapeutic options. Oral administration is the preferred route.

However, oral delivery of peptide drugs has been a long-standing challenge due to their poor bioavailability and degradation in the gastrointestinal tract.

Co-formulation with permeation enhancers to decrease epithelial barrier resistance is a viable strategy to reach systemic circulation but is hampered by low and variable bioavailability, unclear mechanisms of action, and trial-and-error dosage form design approaches.

In this project, we aim to design novel permeation enhancers tailored to disease-specific peptide drug molecules by employing high-throughput cell morphological analysis, advanced modeling, simulation, and biophysical techniques that are integrated into a machine-learning framework.

These efforts provide knowledgebase design of orally administered dosage forms for peptides, ultimately improving the effectiveness and efficiency of oral peptide drug delivery, leading to more robust disease treatment and better patient outcomes.