The role of the bile acid chenodeoxycholic acid in the targeted oral delivery of the anti-diabetic drug gliclazide, and its applications in type 1 diabetes

Artif Cells Nanomed Biotechnol. 2016 Sep;44(6):1508-19. doi: 10.3109/21691401.2015.1058807. Epub 2015 Jul 25.

Abstract

Gliclazide (G) is used to treat type 2 diabetes (T2D), and also has anti-platelet, anti-radical, and anti-inflammatory effects. G has poor water solubility and high inter-individual variations in absorption, limiting its application in type 1 diabetes (T1D). The bile acid, chenodeoxycholic acid (CDCA), has permeation-enhancing effects. Sodium alginate (SA) was used to microencapsulate G and CDCA to produce control (G-SA) and test (G-CDCA-SA) microcapsules. Both microcapsules showed uniform structure, morphology, and good stability profiles. CDCA reduced G-release at pH 7.8, while G-release was negligible at lower pH values in both microcapsules. CDCA incorporation resulted in less swelling and stronger microcapsules, suggesting improved stability.

Keywords: artificial cell microencapsulation; bile acids; chenodeoxycholic acid; diabetes; gliclazide.

MeSH terms

  • Administration, Oral
  • Alginates / chemistry
  • Alginates / pharmacokinetics
  • Alginates / pharmacology
  • Capsules
  • Chenodeoxycholic Acid* / chemistry
  • Chenodeoxycholic Acid* / pharmacokinetics
  • Chenodeoxycholic Acid* / pharmacology
  • Diabetes Mellitus, Type 1 / drug therapy*
  • Drug Compounding
  • Gliclazide* / chemistry
  • Gliclazide* / pharmacokinetics
  • Gliclazide* / pharmacology
  • Glucuronic Acid / chemistry
  • Glucuronic Acid / pharmacokinetics
  • Glucuronic Acid / pharmacology
  • Hexuronic Acids / chemistry
  • Hexuronic Acids / pharmacokinetics
  • Hexuronic Acids / pharmacology
  • Humans
  • Hypoglycemic Agents* / chemistry
  • Hypoglycemic Agents* / pharmacokinetics
  • Hypoglycemic Agents* / pharmacology

Substances

  • Alginates
  • Capsules
  • Hexuronic Acids
  • Hypoglycemic Agents
  • Chenodeoxycholic Acid
  • Glucuronic Acid
  • Gliclazide