Microparticles based on alginate/chitosan/casein three‐dimensional system for oral insulin delivery

Abstract

In the past, oral insulin has been developed to reduce the suffering of diabetic patients. However, the physiological barriers in gastrointestinal (GI) tract are the major challenges in oral delivery of insulin. In this study, a novel oral delivery system of insulin called NiM (NPs in MPs) has been developed to overcome the GI barriers, which based on a three‐dimensional system of biocompatible chitosan/alginate/casein. Alginate/chitosan nanoparticles (AC‐NPs) were firstly prepared by ionic pre‐gel method and complexation with polyelectrolytes. Then, they were subsequently coated with casein as a protective agent to form NiM, which could keep stability and physiological activity of insulin in gastric tract. The characterization of NiM showed stable hydrodynamic parameters, and the entrapment efficiency of insulin reached 51.1%. In vitro, only 13.5% of insulin was released in the simulated gastric fluid for the first 2 h. But about 57.4% of insulin was slowly released in the simulated intestinal fluid for 10 h. These results indicated that the coating of casein could increase stability of insulin in gastric tract and control release of insulin in intestinal tract. Furthermore, NiM provided a sustained and significant reduction of the blood glucose levels of diabetic mice. Overall, the results demonstrated that our formed NiM may be a promising oral delivery system of insulin for diabetic patients.

Insulin-Loaded Soybean Trypsin Inhibitor-Chitosan Nanoparticles: Preparation, Characterization, and Protective Effect Evaluation

“…TEM was used to evaluate the morphological characteristics of INs-STI-CS nanoparticles. In this method, an insulin-loaded nanoparticle solution (10 μL) was moved onto a carbon-coated copper grid, and the sample was viewed and photographed with a Tecnai Spirit D1319 transmission electron microscope at an accelerated voltage of 80 kV [ 5 ].…”

“…Insulin, a polypeptide hormone secreted by pancreatic cells in vertebrates, exerts hypoglycemic effects [ 1 , 5 ]. Since insulin was discovered by Canadians F.G. Banting and C.H.…”

“…Therefore, to effectively control diabetes, there is an urgent need to find a painless and convenient method of insulin administration. In recent years, considerable research efforts have been directed toward oral insulin delivery due to its ability to mimic the endogenous insulin pathway and provide better glucose homeostasis effects [ 5 ]. The oral route represents the most convenient and widely employed approach for insulin administration, demonstrating excellent patient compliance [ 5 ].…”

“…In recent years, considerable research efforts have been directed toward oral insulin delivery due to its ability to mimic the endogenous insulin pathway and provide better glucose homeostasis effects [ 5 ]. The oral route represents the most convenient and widely employed approach for insulin administration, demonstrating excellent patient compliance [ 5 ]. However, insulin is pH/protease sensitive, and orally administrated insulin is susceptible to degradation and loss of activity before reaching systemic circulation, which makes its oral bioavailability extremely low [ 10 ].…”

Formulation and Evaluation of Insulin-Loaded Sodium-Alginate Microparticles for Oral Administration

“…The two most investigated natural polymers are alginate and chitosan. In recent years, several studies have investigated different alginate-based insulin formulations that seem promising for increasing the oral bioavailability of insulin [ 16 , 17 , 18 , 19 ]. The great benefit of sodium-alginate lies in its status a non-toxic, biocompatible and biodegradable polysaccharide.…”