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Designing GLP-1 delivery: structural perspectives and formulation approaches for optimized therapy
Ravi Vamsi Peri1, Harsh Anchan2, Kamal Jonnalagadda2
1Department of Pharmaceutical Sciences, Philadelphia College of Pharmacy, Saint Joseph's University, Philadelphia, PA, USA. periravivamsi@gmail.com.
Nutrition & Diabetes
|November 23, 2025
Summary
Glucagon-like peptide-1 (GLP-1) analogs offer dual benefits for metabolic disorders, combining blood sugar control with weight loss. Modifications and advanced delivery enhance their therapeutic effectiveness and duration.
Area of Science:
- Endocrinology and Metabolism
- Pharmacology and Pharmaceutical Sciences
Background:
- Glucagon-like peptide-1 (GLP-1) is a key hormone for metabolic regulation, but its clinical use is limited by rapid degradation by dipeptidyl peptidase-IV (DPP-IV).
- Short half-life and instability pose challenges for effective therapeutic application of native GLP-1 in managing metabolic disorders.
Purpose of the Study:
- To review the origin, secretion, and limitations of GLP-1.
- To explore diverse modification strategies and delivery systems designed to enhance the pharmacokinetic profile and efficacy of GLP-1 analogs.
- To provide insights into developing improved treatments for metabolic disorders.
Main Methods:
- Exploration of GLP-1's physiological role and degradation pathways.
- Review of various chemical modification techniques: N and C-terminal modifications, fatty acid side chain modifications, and large molecule conjugation.
- Analysis of optimized delivery strategies for sustained and controlled release of GLP-1 analogs.
Main Results:
- Structural modifications significantly improve GLP-1 analog half-life, stability, receptor binding affinity, and bioactivity.
- Fatty acid conjugation and large molecule conjugation are effective strategies for prolonging GLP-1 analog action.
- Optimized delivery systems are crucial for achieving sustained therapeutic effects.
Conclusions:
- Chemical modifications and advanced delivery systems have successfully overcome the limitations of native GLP-1.
- GLP-1 analogs represent a promising therapeutic avenue for metabolic disorders, offering both glycemic control and weight management.
- Continued research in this area holds potential for developing more effective and patient-friendly treatments for metabolic health.
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