4.3 Article

In Vitro and in Vivo Comparative Study of Oral Nanoparticles and Gut Iontophoresis as Oral Delivery Systems for Insulin

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BIOLOGICAL & PHARMACEUTICAL BULLETIN
卷 44, 期 2, 页码 251-258

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PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/bpb.b20-00737

关键词

insulin; nanoparticle; gut iontophoresis; oral delivery

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An advanced gut iontophoresis technology has been developed for delivering insulin nanoparticles across the gut wall, showing promising results in enhancing insulin transport and inducing intense hypoglycemic effects. Cell viability assays confirmed the non-toxic effects of nanoparticles on intestinal cells, suggesting that nanoparticle gut iontophoresis could be a potential non-invasive technique for oral insulin delivery.
Multiple daily injections of insulin for diabetes cause mane hazards for diabetic patients. Oral non-invasive insulin delivery could be more convenient and less painful than parenteral route. In past decades transdermal iontophoresis had been studied for insulin delivery across the skin with or without chemical permeation enhancers. However, the results of these studies were not efficacious and serum insulin levels were not therapeutically effective. In the present study an advanced technology gut iontophoresis for insulin delivery across the gut wall was compared with traditional oral insulin delivery in the form of nanoparticles. In vitro application of electric current to the intestinal membrane could enhance the Ilux of insulin nanoparticles (3.4 fold enhancement of insulin transport) from the donor to the receptor compartment in the Franz cell. In vivo iontophoresis of insulin nanoparticles through the gut wall would produce intense hypoglycemia (57% glycemia drop in 3h) without damage of the intestinal tissues. Cell viability assay indicated that 50-500 mu g/mL nanoparticles had no toxic effect on Caco-2 cells. Nanoparticles gut iontophoresis could be a promising non-invasive technique for oral insulin delivery.

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