Labelled polycyanoacrylate nanoparticles for human in vivo use.

Isobutyl and isohexyl cyanoacrylate nanoparticles are used as drug carriers, particularly for some anti-cancer drugs. Body distribution as well as pharmacokinetics have been well studied in animal and partially in man. Labelling of the monomer itself or of the carried drug with beta-emitters allowed such studies. In man, however, organ distribution and uptake could easily be done and followed by means of scintigraphy (imaging) techniques if one could achieve nanoparticle labelling with gamma-emitting isotopes. We have developed labelling methods able to supply such carriers using gamma-emitters like radioactive iodine (125I or 131I), indium or technetium. We used DTPA as a spacer in order to fix the last two isotopes. This would mean that any other gamma-emitting cation can theoretically be tried pending on its ability to be chelated by DTPA. The preparations were obtained with high labelling yields, usually > 80% and were relatively stable in human plasma over the whole period of investigation. 111In and 99mTc labelled forms have been administered to rabbit and then to man with 60-75% accumulation in the reticulo-endothelial system.