Eudragit®-based microcapsules of probucol with a gut-bacterial processed secondary bile acid

Ther Deliv. 2018 Nov;9(11):811-821. doi: 10.4155/tde-2018-0036.

Abstract

Aim: Deoxycholic acid (DCA) has improved gliclazide oral absorption, while Eudragit® (ED) polymers have improved formulation stability of antidiabetic drugs. The aim of the study is to test if DCA and ED encapsulation will optimize the release and stability of the potential antidiabetic drug probucol (PB).

Materials & methods: The PB formulations were prepared using ED polymers and DCA, and formulations were analyzed for their rheological and biological properties.

Results: Rheological properties and size distribution were similar among all groups. β-cell survival and biological activities were best with NM30D microcapsules. The inflammatory profile and oxidative stress effects of microcapsules remained similar among all groups.

Conclusion: ED NM30D and DCA incorporation can exert positive and stabilizing effects on PB oral microcapsules.

Keywords: deoxycholic acid; microencapsulation; probucol.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Animals
  • Antioxidants / administration & dosage*
  • Antioxidants / pharmacokinetics
  • Biological Availability
  • Capsules
  • Cell Line
  • Cell Survival / drug effects
  • Deoxycholic Acid / chemistry
  • Drug Carriers / chemistry*
  • Drug Compounding / methods
  • Drug Evaluation, Preclinical
  • Drug Liberation
  • Hydrophobic and Hydrophilic Interactions
  • Hypoglycemic Agents / administration & dosage*
  • Hypoglycemic Agents / pharmacokinetics
  • Insulin-Secreting Cells / drug effects*
  • Insulin-Secreting Cells / metabolism
  • Mice
  • Oxidative Stress / drug effects
  • Polymethacrylic Acids / chemistry
  • Probucol / administration & dosage*
  • Probucol / pharmacology

Substances

  • Antioxidants
  • Capsules
  • Drug Carriers
  • Hypoglycemic Agents
  • Polymethacrylic Acids
  • Deoxycholic Acid
  • methylmethacrylate-methacrylic acid copolymer
  • Probucol