Preparation of liposomes entrapping a high specific activity of 111In3+-bound inulin.

Targeting liposomes to specific tissues or cells require the unequivocal determination of the uptake of liposomes at the cellular level. The present report describes the preparation of liposomes entrapping a high specific activity of 111In3+-bound inulin, and the potential applications of a multiple labeling technique for characterizing the extent of uptake of liposomes by tissues or different cells in a given tissue in vivo. The labeling method involves the application of the technique of acetylacetone-mediated, ionophoric loading of 111In3+ into liposomes entrapping an inulin derivative to which a strong chelating agent, diethylenetriamine-pentaacetic acid (DTPA), is bound. Subsequent ionophoric removal of the weakly bound 111In3+ by incubating the previously 111In3+-loaded liposomes with 10 mM nitrilotriacetic acid and 100 microM tropolone at room temperature for 20 min results in the preparation of liposomes entrapping 111In3+-DTPA-inulin. Our method of preparation yields net efficiencies of converting 63-78% of the externally added 111In3+ to liposome-entrapped 111In3+-DTPA-inulin.