Inclusion complex based on N-acetyl-L-cysteine and arginine modified hydroxypropyl-β-cyclodextrin for oral insulin...

Area of Science:

• Biomaterials Science
• Drug Delivery Systems
• Nanotechnology

Background:

• Subcutaneous insulin injection is standard for diabetes mellitus but lacks patient compliance.
• Oral insulin delivery offers a minimally invasive, patient-friendly alternative.
• Developing effective oral insulin carriers remains a significant challenge.

Purpose of the Study:

• To synthesize and characterize a novel polymer carrier for oral insulin delivery.
• To evaluate the protective and transport capabilities of the novel carrier.
• To assess the in vivo hypoglycemic efficacy of orally delivered insulin using the carrier.

Main Methods:

• Synthesis and characterization of N-acetyl-L-cysteine and arginine modified hydroxypropyl-β-cyclodextrin (NAC-HP-β-CD-Arg).
• Formation of NAC-HP-β-CD-Arg@insulin complex.
• In vitro enzymatic degradation, mucin binding, and Caco-2 cell transport studies.
• In vivo hypoglycemic effect evaluation in diabetic rats.

Main Results:

• Successful synthesis and characterization of NAC-HP-β-CD-Arg.
• NAC-HP-β-CD-Arg demonstrated protective effects against insulin enzymolysis.
• Enhanced mucin binding and significantly improved insulin transport across Caco-2 cells compared to free insulin.
• Orally administered NAC-HP-β-CD-Arg@insulin achieved excellent and sustained hypoglycemic effects in diabetic rats.

Conclusions:

• NAC-HP-β-CD-Arg is a viable carrier for oral insulin delivery.
• The developed system offers a promising strategy for improving diabetes management.
• This approach enhances insulin stability and bioavailability for oral administration.