Oral Liraglutide Nanoparticles: Chitosan-Coated Delivery System Provides Sustained Blood Sugar Control | Research

The takeaway

Zein/Eudragit-chitosan nanoparticles delivered liraglutide orally with sustained release and glycemic control, potentially replacing daily injections with an oral pill.

Oral GLP-1 delivery
Zein/Eudragit-chitosan nanoparticles protect liraglutide from stomach acid and deliver it orally with sustained glycemic control

What the researchers found

Zein/Eudragit-chitosan nanoparticles protected liraglutide from gastric degradation, provided sustained oral delivery, and achieved effective glycemic control in animal models.

Why it matters

Liraglutide injection is a barrier to patient adherence. An oral nanoparticle formulation could make this effective GLP-1 drug as easy as taking a pill, dramatically expanding its use.

The numbers in context

Oral nanoparticle formulation achieved comparable pharmacokinetic and glycemic outcomes to subcutaneous injection in diabetic rats.

How the study worked

Formulated liraglutide-loaded zein/Eudragit nanoparticles coated with chitosan. Characterized particle size, encapsulation, release kinetics, acid stability, and in vivo glycemic control.

Who was studied

T2DM rats comparing oral LIRA nanoparticles vs. subcutaneous LIRA injection

What this study cannot tell us

Animal study — human GI conditions and absorption may differ. Bioavailability compared to injection needs quantification. Manufacturing scalability and cost of nanoparticles need assessment.

How to read the evidence

Preliminary evidence: formulation study with in vivo glycemic control in animals. Human pharmacokinetics and bioavailability not established.

When this study was published

Published in 2024. Advances oral peptide delivery technology for GLP-1 drugs.

The bigger picture

Oral delivery of peptide drugs is one of pharmaceutical science's biggest challenges. While oral semaglutide (Rybelsus) uses a different approach (SNAC enhancer), nanoparticle-based delivery could offer sustained release profiles that are difficult to achieve with enhancer technology, potentially enabling once-daily or even less frequent oral GLP-1 therapy.

Questions still open

How does oral nanoparticle liraglutide bioavailability compare to injectable liraglutide?
Could this nanoparticle platform deliver other peptide drugs orally?
What is the manufacturing cost comparison with current injection formulations?

Common questions

Could liraglutide become an oral pill?

This study shows that nanoparticle technology can protect liraglutide from stomach acid and deliver it through the intestines with sustained release. While not yet available as a product, this technology could eventually enable oral liraglutide pills.

How do the nanoparticles protect liraglutide?

The nanoparticles use three layers of protection: zein (corn protein) forms the core, Eudragit provides acid resistance in the stomach, and chitosan coating promotes adhesion to intestinal walls for absorption. Together, they shield liraglutide until it reaches the right part of the gut.

Read the original research

Oral Delivery of Liraglutide-Loaded Zein/Eudragit-Chitosan Nanoparticles Provides Pharmacokinetic and Glycemic Outcomes Comparable to Its Subcutaneous Injection in Rats.

Pharmaceutics, 16(5)

View on PubMed ↗Publisher’s paper ↗

Citation

Ziebarth, Jeferson; da Silva, Letícia Marina; Lorenzett, Ariane Krause Padilha; Figueiredo, Ingrid Delbone; Carlstrom, Paulo Fernando; Cardoso, Felipe Nunes; de Freitas, André Luiz Ferreira; Baviera, Amanda Martins; Mainardes, Rubiana Mara. (2024). Oral Delivery of Liraglutide-Loaded Zein/Eudragit-Chitosan Nanoparticles Provides Pharmacokinetic and Glycemic Outcomes Comparable to Its Subcutaneous Injection in Rats.. Pharmaceutics, 16(5). https://doi.org/10.3390/pharmaceutics16050634