An enteric-coated dry emulsion formulation for oral insulin delivery

Influence of magnesium stearate on the physicochemical and pharmacodynamic characteristics of insulin-loaded Eudragit entrapped mucoadhesive microspheres

“…A more efficient reduction in the blood glucose level could have masked this initial increase in other animals. A prominent anti-hyperglycemic effect was noticed with batches C 1 and C 4 formulations from 4 and 2 h respectively, and the effect was visible up to 12 h. This is an indication that the microspheres protected insulin against proteolytic degradation in the GIT, consistent with previous reports (Tiyaboonchai, 2003;Nakamura et al, 2004;Toorisaka et al, 2005). The maximum plasma glucose reduction from the baseline was found to be 64 mg/dl and the time to reach the maximum plasma glucose reduction was 12 h. Orally administered insulin solution, distilled water and unloaded microspheres preparation (C 0 ) (serving as negative controls) showed a general increase in the blood glucose level unlike subcutaneously administered insulin that served as positive control.…”

“…The oral route is considered to be the most convenient, acceptable and desired route of drug delivery which will help eliminate the pain caused by injection, psychological barrier associated with multiple daily injection and possible infections (Kisel et al, 2001;Kim & Peppas, 2003;Whitehead et al, 2004;Cui et al, 2006;Sarmento et al, 2007). Oral delivery of insulin as a non-invasive therapy for diabetes mellitus is still a challenge to the drug delivery technology, due to low oral bioavailability, lack of lipophility, poor permeability across intestinal epithelium because of insulin high molecular weight as well as digestion by proteolytic enzymes in the luminal cavity (Tozaki, 2001; Gowthamarajan & Kulkarni, 2003;Tiyaboonchai, 2003;Krauland et al, 2004;Li & Deng, 2004;Nakamura et al, 2004;Toorisaka et al, 2005;Sajeesh & Sharma, 2006;Sarmento, 2006;Tuesca & Lowman, 2006;Lin, 2007;Simon, 2007).…”

Enhanced oral bioavailability of insulin-loaded solid lipid nanoparticles: pharmacokinetic bioavailability of insulin-loaded solid lipid nanoparticles in diabetic rats

“…Another major barrier to the absorption of hydrophilic macromolecules like insulin is that they cannot diffuse across epithelial cells through lipid-bilayer cell membranes to the blood stream (Lin et al, 2007). In other words, insulin has low permeability through the intestinal mucosa (Toorisaka et al, 2005). High molecular weight and lack of lipophilicity of insulin causes poor permeability across intestinal epithelium.…”

Polysaccharides in Oral Drug Delivery — Recent Applications and Future Perspectives

“…Eudragit ® L, S, FS) to cellulose esters like C-A-P, HPMCP, cellulose acetate trimellitate and hydroxypropyl methylcellulose acetate succinate (HPMCAS) 13,14 . Recently, various formulations for oral protein/peptide delivery have been described in the literature, amongst them an enteric-coated dry emulsion formulation for oral insulin delivery 15 . This edible insulin formulation is a dry microparticulate emulsion with enteric properties and consists of a surfactant, a vegetable oil, and HPMCP as the pH-responsive polymer.…”

“…This edible insulin formulation is a dry microparticulate emulsion with enteric properties and consists of a surfactant, a vegetable oil, and HPMCP as the pH-responsive polymer. In an in vitro study, the insulin release from the formulation was shown to respond to the change in external environment in the gastrointestinal tract 15 . Overall, the study results suggest that this new enteric emulsion formulation could potentially be applied to oral delivery of several kinds of pharmaceutical peptides and proteins.…”