Oral insulin delivery: existing barriers and current counter-strategies

J Pharm Pharmacol. 2018 Feb;70(2):197-213. doi: 10.1111/jphp.12852. Epub 2017 Nov 28.

Abstract

Objectives: The chronic and progressive nature of diabetes is usually associated with micro- and macrovascular complications where failure of pancreatic β-cell function and a general condition of hyperglycaemia is created. One possible factor is failure of the patient to comply with and adhere to the prescribed insulin due to the inconvenient administration route. This review summarizes the rationale for oral insulin administration, existing barriers and some counter-strategies trialled.

Key findings: Oral insulin mimics the physiology of endogenous insulin secreted by pancreas. Following the intestinal absorption of oral insulin, it reaches the liver at high concentration via the portal vein. Oral insulin on the other hand has the potential to protect pancreatic β-cells from autoimmune destruction. Structural modification, targeting a particular tissue/receptor, and the use of innovative pharmaceutical formulations such as nanoparticles represent strategies introduced to improve oral insulin bioavailability. They showed promising results in overcoming the hurdles facing oral insulin delivery, although delivery is far from ideal.

Summary: The use of advanced pharmaceutical technologies and further research in particulate carrier system delivery predominantly nanoparticle utilization would offer useful tools in delivering insulin via the oral route which in turn would potentially improve diabetic patient compliance to insulin and the overall management of diabetes.

Keywords: diabetes; formulation; insulin; oral; tablet.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Biological Availability
  • Biomarkers / blood
  • Blood Glucose / drug effects*
  • Blood Glucose / metabolism
  • Diabetes Mellitus / blood
  • Diabetes Mellitus / diagnosis
  • Diabetes Mellitus / drug therapy*
  • Drug Carriers
  • Drug Compounding
  • Drug Delivery Systems*
  • Humans
  • Hypoglycemic Agents / administration & dosage*
  • Hypoglycemic Agents / adverse effects
  • Hypoglycemic Agents / pharmacokinetics
  • Insulin / administration & dosage*
  • Insulin / adverse effects
  • Insulin / pharmacokinetics
  • Intestinal Absorption
  • Nanoparticles

Substances

  • Biomarkers
  • Blood Glucose
  • Drug Carriers
  • Hypoglycemic Agents
  • Insulin