Abstract
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.
Highlights
Protein-based drugs cover diverse therapeutic indications and are beneficial in the treatment of many incurable diseases [1]
The sequential coating of AC-Ins with glycol-chitosan and Eudragit® S100 increased the size of the nanoparticles and reversed their surface charge
The Fourier transform infrared spectroscopy (FT-IR) spectrum of insulin exhibited amide I peak at 1645 cm−1 and amide II peak at 1515 cm−1
Summary
Protein-based drugs cover diverse therapeutic indications and are beneficial in the treatment of many incurable diseases [1]. The high target-selectivity of protein drugs can reduce undesirable side effects and toxicity [2]. A large amount of research and development has been devoted to biological drugs including proteins and peptides. Protein drugs are primarily administered via parenteral injection because of their low bioavailability [3]. There is a high demand for the non-invasive formulations of protein drugs that can improve patient compliance. Diabetes mellitus (DM) is a chronic metabolic disease that is present in a large portion of the patient population (i.e. more than 415 million adults), and it is predicted to reach 642 million patients by 2040 [4].
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