Background
GLP-1 receptor agonists are highly effective treatments for Type 2 diabetes and obesity, with global demand on the rise. However, the majority are injectable, posing a significant burden on patients and leading to challenges in treatment adherence. While oral GLP-1 medications like oral semaglutide exist, their delivery often requires very high peptide concentrations and specialized absorption enhancers, leading to increased manufacturing costs and formulation complexity. Lonza Capsugel’s dual-layer protection strategy opens a new pathway for enabling the oral delivery of a broader range of peptide therapeutics, particularly GLP-1 peptides.
Key Findings
A team of researchers at Lonza Capsugel has developed and evaluated an innovative “dual-layer protection strategy” to enable the oral delivery of GLP-1 peptides. This proof-of-concept platform demonstrates a promising approach to overcome the longstanding challenge of enzymatic degradation of peptide drugs within the gastrointestinal tract by uniquely combining hydrophobic ion pairing (HIP), lipid-based formulations (LBF), and enteric capsule technology.
The Dual-Layer Protection Strategy: Technical Details
Oral delivery of biologics like GLP-1 peptides has historically been extremely challenging due to their size, susceptibility to digestive enzymes, and low permeability across the gastrointestinal epithelium. Lonza Capsugel’s developed dual-layer protection strategy integrates multiple approaches to address these critical hurdles.
The first protective layer involves Hydrophobic Ion Pairing (HIP). This technique transforms hydrophilic peptide molecules into more hydrophobic complexes, significantly improving their solubility within lipid-based formulations (LBFs).
Secondly, by incorporating these HIP complexes into a Lipid-Based Formulation (LBF), the peptide is shielded from digestive enzymes in the gastrointestinal fluids, thereby enhancing its stability.
Furthermore, this LBF is encapsulated within an enteric capsule. This design ensures the capsule remains intact as it passes through the highly acidic environment of the stomach, releasing the peptide in the more neutral conditions of the small intestine. The small intestine offers a comparatively lower enzymatic activity and more favorable conditions for drug absorption.
In vitro evaluations have demonstrated that this combined approach significantly protects GLP-1 peptides from enzymatic degradation in simulated digestive fluids. This technology lays the foundation for improving in vivo bioavailability and ultimately contributing to the clinical success of oral GLP-1 therapies.
Industry Impact and Future Outlook
The promising in vitro results of this dual-layer protection strategy pave the way for future in vivo animal studies and human clinical trials. If confirmed for in vivo bioavailability and therapeutic efficacy, this platform could be broadly applicable not only to GLP-1 peptides but also to the oral delivery of various other therapeutic peptides.
Lonza Capsugel aims to further develop this technology and collaborate with pharmaceutical partners to bring more oral peptide therapeutics to market. This advancement represents a crucial step in diversifying biopharmaceutical administration routes and reinforcing a patient-centric direction in drug discovery. Ultimately, success means eliminating the need for injections, greatly enhancing patient convenience, and potentially increasing treatment adherence. This initiative serves as a concrete example of how innovation in Drug Delivery System (DDS) technologies can contribute to patient-centered healthcare.
Source: https://www.capsugel.com/knowledge-center/pharma/capsules/oral-glp1-delivery-enteric-capsules
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