A liposomal MRI contrast agent: phosphatidylethanolamine-DTPA

The chelating agent, diethylenetriaminepentaacetic acid (DTPA), was attached via one -COOH group to the amino headgroup of phosphatidylethanolamine to produce a phospholipid which is also a powerful chelating agent. It readily assembles into the walls of lipid bilayer structures as a liposome-associated carrier of cations for MR contrast or radioisotope studies. Freeze-etch electron microscopy showed that phosphatidylethanolamine-DTPA formed satisfactory sonicated vesicles when mixed with natural phospholipids at up to 50 wt%. The resultant structures with bound gadolinium effectively shortened T1 and T2 of surrounding water protons. When sonicated liposomes bearing chelating agent with bound 111In3+ were injected intravenously into rats, uptake was primarily by liver and spleen. By 24 h postinjection there was biliary excretion of this material. Phosphatidylethanolamine-DTPA may have some general utility as an amphiphilic liposomal chelating agent for polyvalent cations.