Montmorillonite intercalated with glutathione for antioxidant delivery: synthesis, characterization, and bioavailability evaluation

Int J Pharm. 2012 Apr 4;425(1-2):29-34. doi: 10.1016/j.ijpharm.2012.01.015. Epub 2012 Jan 14.


A most powerful antioxidant, glutathione (GSH), plays an important role in detoxification, immune response, and protection against reactive oxygen species. However, orally ingested GSH can be easily degradable to free amino acids by chemical and enzymatic hydrolysis, resulting in low bioavailability. The aim of this study was, therefore, to enhance GSH bioavailability by developing GSH-montmorillonite (MMT) hybrid system. It was also coated with polyvinylacetal diethylaminoacetate (AEA) for better stability. Both GSH-MMT and AEA-GSH-MMT hybrids were characterized by powder X-ray diffraction (PXRD), Fourier transformed infrared (FT-IR), and thermogravimetric analysis (TGA), indicating that GSH was successfully intercalated into the interlayer spaces of MMT. In vivo antioxidant activity assay revealed that AEA-GSH-MMT hybrid significantly increased antioxidant activity in the plasma after oral administration in mice. Pharmacokinetic study also indicated that AEA-GSH-MMT hybrid considerably increased the plasma concentration of GSH at 1h post-oral administration. Moreover, both the hybrid systems remarkably enhanced GSH delivery to the main target tissue, liver. All the results suggest that GSH-MMT hybrid systems have great potential to enhance bioavailability of oral GSH, providing new insight into their pharmaceutical application.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antioxidants / administration & dosage
  • Antioxidants / chemistry*
  • Antioxidants / pharmacokinetics
  • Bentonite / administration & dosage
  • Bentonite / chemistry*
  • Bentonite / pharmacokinetics
  • Benzothiazoles / metabolism
  • Biological Availability
  • Drug Carriers / administration & dosage
  • Drug Carriers / chemistry*
  • Drug Carriers / pharmacokinetics
  • Drug Stability
  • Glutathione / administration & dosage
  • Glutathione / chemistry*
  • Glutathione / pharmacokinetics
  • Male
  • Mice
  • Mice, Inbred ICR
  • Polyvinyls / administration & dosage
  • Polyvinyls / chemistry*
  • Polyvinyls / pharmacokinetics
  • Powder Diffraction
  • Spectroscopy, Fourier Transform Infrared
  • Sulfonic Acids / metabolism
  • Thermogravimetry
  • Tissue Distribution
  • X-Ray Diffraction


  • Antioxidants
  • Benzothiazoles
  • Drug Carriers
  • Polyvinyls
  • Sulfonic Acids
  • polyvinylacetal diethylaminoacetate
  • Bentonite
  • 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid
  • Glutathione