pH-sensitive chitosan/alginate core-shell nanoparticles for efficient and safe oral insulin delivery

Area of Science:

• Biomaterials Science
• Nanotechnology
• Pharmaceutical Sciences

Background:

• Oral insulin administration faces challenges due to enzymatic degradation and poor absorption in the gastrointestinal tract.
• Developing effective oral insulin delivery systems is crucial for improving patient compliance and therapeutic outcomes.
• Chitosan-alginate nanoparticles offer potential as a protective carrier for biopharmaceuticals.

Purpose of the Study:

• To develop and evaluate chitosan-alginate (CS/ALG) core-shell nanoparticles for oral insulin delivery.
• To investigate the physicochemical properties, in vitro release, and in vivo efficacy of the CS/ALG nanoparticles.
• To assess the safety profile of the CS/ALG nanoparticles for oral administration.

Main Methods:

• Chitosan-alginate nanoparticles were prepared using ionotropic pre-gelation and polyelectrolyte complexation.
• Particle size, morphology, and insulin encapsulation efficiency were characterized using dynamic light scattering (DLS) and other techniques.
• In vitro release studies were conducted under simulated gastric and intestinal conditions.
• In vivo studies evaluated hypoglycemic effects and insulin bioavailability in an animal model.

Main Results:

• CS/ALG nanoparticles exhibited an average particle size of 100-200 nm with a spherical or sub-spherical shape.
• High insulin encapsulation efficiency (approximately 85%) was achieved.
• The nanoparticles demonstrated pH-sensitive release, retaining insulin in simulated gastric conditions and releasing it in simulated intestinal conditions.
• In vivo studies showed significant hypoglycemic effects and improved insulin-relative bioavailability (approximately 8.11%) with no systemic toxicity.

Conclusions:

• Chitosan-alginate core-shell nanoparticles are effective carriers for oral insulin delivery.
• The mild preparation process and pH-sensitive nature contribute to enhanced insulin bio-efficiency.
• These nanoparticles represent a promising and safe platform for oral insulin administration.