Abstract: Methods and compositions are provided for the treatment of inflammation and disorders, diseases, and adverse conditions, i.e., pathologies, caused by or otherwise associated with inflammatory processes. A metal ion sequestering agent that directly or indirectly exerts an anti-inflammatory effect is administered to a subject in combination with a sequestration inactivating moiety that facilitates transport of the metal ion sequestering agent through biological membranes. The sequestration inactivating moiety also inactivates the metal ion sequestering agent until association between the two components is cleaved in vivo to release the active sequestering agent. Compositions containing a metal ion sequestering agent and a sequestration inactivating moiety are also provided; the compositions optionally contain an added anti-inflammatory agent.