Stability and biological testing of taurine-conjugated bile acid antioxidant microcapsules for diabetes treatment

Ther Deliv. 2019 Feb;10(2):99-106. doi: 10.4155/tde-2018-0034.

Abstract

Aim: Taurine-conjugated bile acids possess positive formulation-stabilization effects, which are desirable in diabetes treatments. The taurine-conjugated bile acid, taurocholic acid (TCA), has shown promising formulation-stabilizing effects on the delivery of the antioxidant drug, probucol (PB), but success is limited due to its poor release profile. This study aimed to design new PB-TCA formulations using new polymers, and examine antioxidant and antidiabetic effects using β-cells for PB with or without TCA.

Materials and methods: Different formulations using alginate-insoluble esters of polymethylacrylate polymers encapsulating PB and TCA were developed, microencapsulated and examined for stability and biological activity.

Results: TCA addition to new PB matrices improved osmotic and mechanical properties, and this effect was dependent on polymethylacrylate composition and concentration.

Conclusion: TCA can optimize the oral delivery of anti-diabetic compounds.

Keywords: diabetes mellitus; eudragit; microencapsulation; oral delivery; probucol; taurocholic acid.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alginates / chemistry
  • Animals
  • Antioxidants / chemistry*
  • Antioxidants / metabolism
  • Antioxidants / pharmacology
  • Antioxidants / therapeutic use
  • Bile Acids and Salts / chemistry*
  • Capsules / chemistry*
  • Cell Line
  • Diabetes Mellitus / drug therapy
  • Drug Compounding
  • Drug Stability
  • Humans
  • Mice
  • Oxidative Stress / drug effects
  • Probucol / chemistry*
  • Probucol / metabolism
  • Probucol / pharmacology
  • Probucol / therapeutic use
  • Taurine / chemistry*

Substances

  • Alginates
  • Antioxidants
  • Bile Acids and Salts
  • Capsules
  • Taurine
  • Probucol