Enhanced oral delivery of insulin via the colon-targeted nanocomposite system of organoclay/glycol chitosan/Eudragit®S100

This study aimed to develop a ternary nanocomposite system of organoclay, glycol-chitosan, and Eudragit®S100 as an effective colon targeted drug delivery carrier to enhance the oral absorption of insulin. A nanocomplex of insulin and aminoclay was prepared via spontaneous co-assembly, which was then coated with glycol-chitosan and Eudragit S®100 (EGAC-Ins). The double coated nanocomplex, EGAC-Ins demonstrated a high entrapment efficiency of greater than 90% and a pH-dependent drug release. The conformational stability of insulin entrapped in EGAC-Ins was effectively maintained in the presence of proteolytic enzymes. When compared to a free insulin solution, EGAC-Ins enhanced drug permeability by approximately sevenfold in Caco-2 cells and enhanced colonic drug absorption in rats. Accordingly, oral EGAC-Ins significantly reduced blood glucose levels in diabetic rats while the hypoglycemic effect of an oral insulin solution was negligible. In conclusion, EGAC-Ins should be a promising colonic delivery system for improving the oral absorption of insulin.

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or continue reading here: Lee, S.H., Back, S., Song, J.G. et al. Enhanced oral delivery of insulin via the colon-targeted nanocomposite system of organoclay/glycol chitosan/Eudragit®S100. J Nanobiotechnol 18, 104 (2020). https://doi.org/10.1186/s12951-020-00662-x

Conclusion
In this study, a colon-targeted ternary nanocomposite system composed of organoclay/glycol-chitosan/Eudragit® S100 was developed to enhance the oral delivery of insulin. EGAC-Ins, an insulin-loaded ternary nanocomposite formulation, was obtained as nano-sized particles with high entrapment efficiency (> 90%). EGAC-Ins displayed pH-dependent drug release characteristics that minimized premature drug release in the upper GI tract. The conformational stability of insulin entrapped in EGAC-Ins was preserved in simulated gastrointestinal fluids. In addition to the enhanced cell permeability and colonic absorption of insulin in rats via EGAC-Ins, orally-administered EGAC-Ins significantly improved the hypoglycemic effect in diabetic rats while the efficacy of oral insulin solution was negligible. Taken together, the present study suggests that EGAC-Ins might be useful to enhance the bioavailability and efficacy of oral insulin.