Characterization and optimization of de‐esterified Tragacanth‐chitosan nanocomposite as a potential carrier for oral delivery of insulin: In vitro and ex vivo studies

• Published in: Journal of biomedical materials research. Part A 2021-11, Vol.109 (11), p.2164-2172
• Main Authors: Shirzadian, Touraj, Nourbakhsh, Mohammad Sadegh, Fattahi, Ali, Bahrami, Gholamreza, Mohammadi, Ghobad
• Format: Article
• Language: English
• Subjects: Administration, Oral; Animals; Chemical synthesis; Chitosan; Chitosan - chemistry; Chitosan - pharmacology; Coacervation; Drug Carriers - chemistry; Drug Carriers - pharmacology; Esterification; Fourier analysis; Fourier transforms; Gravimetric analysis; Humans; Infrared analysis; Insulin; Insulin - chemistry; Insulin - pharmacokinetics; Insulin - pharmacology; Male; Molecular weight; Nanocomposites; Nanocomposites - chemistry; Nanocomposites - therapeutic use; Nanoparticles; Optimization; Oral administration; Permeability; Rats; Rats, Wistar; Response surface methodology; Stability analysis; Thermal stability; Tragacanth; Tragacanth - chemistry; Tragacanth - pharmacology; Zeta potential
• ISSN: 1549-3296; 1552-4965
• DOI: 10.1002/jbm.a.37202

Oral administration of insulin is one of the most challenging topics within this area, because insulin is degraded in stomach before it enters the bloodstream. In this study, for the first time, a nano‐carrier for controlled and targeted oral delivery of insulin was developed using de‐esterified Tragacanth and chitosan. The fabricated nanoparticles were synthesized using coacervation technique and their properties were optimized using response surface methodology. The effect of experimental variables on the particle size and loading efficiency was examined. In addition, the interactions between components were analyzed using Fourier transform infrared. The thermal stability of nanoparticles was studied by thermal gravimetric analysis. The insulin loading efficiency was measured and in vitro release profile and ex vivo insulin permeability was determined. Optimized nanoparticles showed spherical shape with a size less than 200 nm and zeta potential of +17 mV. Owing to their nanoscale dimensions and mucoadhesiveness, nanoparticles were synthesized using medium molecular weight of Chitosan. The insulin loading efficacy for the system was 6.4%, released under simulated gastrointestinal conditions in a pH‐dependent manner. Based on all of the obtained results, it can be concluded that these nanoparticles can potentially be utilized as a carrier for the oral insulin delivery.