Studies of radiopharmaceutical-enclosing lipid-protein vesicles formed from native plasma components.

Vesicles 500-600 A in diameter were formed by sonicating diluted samples of rat and mouse plasma. An average preparation of these vesicles formed from 1 ml of plasma contained 7.5 mg of plasma lipid and 7.3 mg of plasma protein. Plasma vesicles could be made to enclose such radiopharmaceuticals as 99mTcO4-, and the vesicles were found to be impermeable to this anion. We have studied the in vivo distribution patterns of 99mTc after intravenous injection into the rat or mouse of pertechnetate-plasma vesicles formed from rat or mouse plasma, and we find that the radioactivity remains primarily within the circulation even at 60 min after injection. In contrast, vesicles formed from artificial lipids are rapidly removed by the liver and spleen. Formation of vesicles from native plasma constituents offers a means of carrying drugs and radiopharmaceuticals in vivo in packages that have a low risk of being either toxic or antigenic.