Insulin delivered orally in polyelectrolytically stable nanoparticles elicits a pharmacological effect

摘要

Hypoglycemic effect and insulinemia of insulin administered orally in polyelectrolytically stablized nanoparticles was evaluated in streptozotocin (STZ)-induced diabetic rats. Nanoparticles with mean diameter < 400 nm were formed by alginate nucleated around calcium and associated with dextran sulfate and poloxamer 188, further stabilized by chitosan and subsequently coated with albumin. Insulin decreased plasma glucose levels to 40% of the basal values with sustained hypoglycemic effect over 24 h, and oral bioavailability of 13% showed a 3-fold increase by comparison with free insulin. Encapsulating insulin in nanoparticles through a simplified method avoiding harsh conditions improved the pharmacological effect of the therapeutic protein, and potentially that of other biopharmaceuticals.