Assessment of methylsulfonylmethane as a permeability enhancer for regional EDTA chelation therapy

Drug Deliv. 2009 Jul;16(5):243-8. doi: 10.1080/10717540902896362.


Pharmacologic chelators do not effectively penetrate cell membranes and blood-brain barrier. This study assesses methylsulfonylmethane (MSM) as a permeability enhancer and an excipient to facilitate EDTA transport across biologic membranes, and to make possible localized, regional chelation. Topical application of MSM with C(14)EDTA onto the rat cornea led to uptake of the C(14)EDTA in all tested ocular tissues. Without MSM, EDTA did not penetrate the eye. The ability of MSM to deliver EDTA into an eye provides an opportunity for regional chelation therapy. Additionally, these studies suggest that MSM could also be an adjuvant for delivering ciprofloxacin and other chemical compounds to specific, local tissue sites.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blood-Brain Barrier / drug effects*
  • Chelating Agents / administration & dosage*
  • Chelating Agents / pharmacology
  • Chelation Therapy*
  • Cornea / drug effects
  • Cornea / metabolism
  • Dimethyl Sulfoxide / administration & dosage*
  • Drug Synergism
  • Edetic Acid / administration & dosage*
  • Edetic Acid / chemistry
  • Eye / drug effects*
  • Eye / metabolism
  • Male
  • Radioisotopes
  • Rats
  • Rats, Sprague-Dawley
  • Sulfones / administration & dosage*


  • Chelating Agents
  • Radioisotopes
  • Sulfones
  • Edetic Acid
  • dimethyl sulfone
  • Dimethyl Sulfoxide