A new approach to labeling cells with technetium-99m, Part I. Preparation of modified polylysine and in vitro cell labeling

A method for labeling cells with technetium-99m via hydrophilic, polycationic poly D-lysine modified by N-acetyl homocysteine has been developed. The modified polylysine (MPL) is labeled with 99mTc in > 95% yield and is stable for > 12 h. Maximum cell labeling is achieved by a 1-h incubation at room temperature with isolated leukocytes, granulocytes and peripheral blood mononuclear cells attaining 60-75% 99mTc incorporation, and red blood cells 35%. Ninety-two percent of the label is retained by leukocytes after a 1-h incubation at room temperature in 50% serum. The cell uptake of 99mTc-MPL is affected by the presence of negatively charged species in the medium; the inhibitory effects of 5% serum or serum albumin can be reversed by increasing the concentration of 99mTc-MPL, while those of heparin are not.