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Labelled polycyanoacrylate nanoparticles for human In Vivo use

1993; Elsevier BV; Volume: 44; Issue: 9 Linguagem: Inglês

10.1016/0969-8043(93)90068-l

1872-9800

G. E. Ghanem, C. Joubran, Roland Arnould, F. Lejeune, J Frühling,

Radiopharmaceutical Chemistry and Applications

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 β-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 γ-emitting isotopes. We have developed labelling methods able to supply such carriers using γ-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 γ-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.