Glucagon-Like Peptide-1 Formulation--the Present and Future Development in Diabetes Treatment

Basic Clin Pharmacol Toxicol. 2016 Mar;118(3):173-80. doi: 10.1111/bcpt.12524. Epub 2015 Dec 28.

Abstract

Type 2 diabetes mellitus is a chronic metabolic disorder that has become the fourth leading cause of death in the developed countries. The disorder is characterized by pancreatic β-cells dysfunction, which causes hyperglycaemia leading to several other complications. Treatment by far, which focuses on insulin administration and glycaemic control, has not been satisfactory. Glucagon-like peptide-1 (GLP1) is an endogenous peptide that stimulates post-prandial insulin secretion. Despite being able to mimic the effect of insulin, GLP1 has not been the target drug in diabetes treatment due to the peptide's metabolic instability. After a decade-long effort to improve the pharmacokinetics of GLP1, a number of GLP1 analogues are currently available on the market. The current Minireview does not discuss these drugs but presents strategies that were undertaken to address the weaknesses of the native GLP1, particularly drug delivery techniques used in developing GLP1 nanoparticles and modified GLP1 molecule. The article highlights how each of the selected preparations has improved the efficacy of GLP1, and more importantly, through an overview of these studies, it will provide an insight into strategies that may be adopted in the future in the development of a more effective oral GLP1 formulation.

Publication types

  • Review

MeSH terms

  • Blood Glucose / metabolism
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Drug Delivery Systems
  • Glucagon-Like Peptide 1 / chemistry
  • Glucagon-Like Peptide 1 / pharmacology*
  • Humans
  • Hyperglycemia / drug therapy
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / pharmacology*
  • Insulin / pharmacology
  • Insulin-Secreting Cells / drug effects
  • Insulin-Secreting Cells / metabolism
  • Nanoparticles / chemistry
  • Postprandial Period

Substances

  • Blood Glucose
  • Hypoglycemic Agents
  • Insulin
  • Glucagon-Like Peptide 1