Oral delivery of peptides : where are we and where are we going ? A review on current strategies and future perspectives.

Details

Supervisors

Beloqui Garcia, Ana

Faculty

Faculté de pharmacie et des sciences biomédicales

Degree label

Master [120] en sciences pharmaceutiques, à finalité spécialisée

Abstract

Peptide therapeutics are known for their specificity, efficacy, and lower toxicity compared to traditional small molecule drugs. The aim of this work is to investigate the factors that contribute to the limited market presence of oral peptide therapeutics, despite the oral route being more favorable to improve patient medication adherence compared to the prevalent injectable route. The factors at fault for the low oral bioavailability are the physicochemical limitations of peptides and the gastrointestinal tract barriers, including the proteolytic gastrointestinal environment, the mucus barrier and the intestinal epithelial barrier. Over the years, several strategies have been developed to overcome these barriers, including utilization of enteric coatings, acidity modifiers, peptidase inhibitors, mucus penetrating agents, mucoadhesive agents and permeation enhancers. Additionally, promising advancements have been made with nanocarrier-based approaches for the development of oral peptide formulations. Despite the efforts to improve stability and permeability through combined strategies, the oral bioavailability remains significantly low, sometimes even less than 1% for certain products. However, the emergence of device-based technologies seems to surpass this bioavailability threshold, offering new perspectives for effective oral peptide delivery.