99mTc/188Re-labelled lipid nanocapsules as promising radiotracers for imaging and therapy: formulation and biodistribution

Abstract

Purpose: This study focuses on a promising carrier system for imaging and therapeutic purposes using lipid nanocapsules. To assess their potential for clinical use, we labelled nanocapsules with (99m)Tc and (188)Re and analysed some kinetic biodistribution parameters after intravenous injection in rats.

Methods: Lipophilic complexes [(99m)Tc/(188)Re(S(3)CPh)(2)(S(2)CPh)] ((99m)Tc/(188)Re-SSS) were encapsulated within the nanoparticles during their manufacture with quantitative yield and satisfactory radiochemical purity. Rats were injected intravenously with 3.7 MBq (99m)Tc/(188)Re-labelled nanocapsules and sacrificed at 5, 15 and 30 min and 1, 2, 4, 8, 12, 16, 20 and 24 h.

Results: Dynamic scintigraphic acquisitions showed predominant hepatic uptake, and ex vivo counting indicated a long circulation time of labelled nanocapsules, with a half-life of 21+/-1 min for (99m)Tc and 22+/-2 min for (188)Re. Very weak urinary elimination was observed, indicating good stability of (99m)Tc and (188)Re labelling.

Conclusion: (99m)Tc/(188)Re-SSS nanocapsules can be obtained with high yield and satisfactory radiochemical purity. The biodistributions of (99m)Tc/(188)Re-labelled nanocapsules are close to those of classical PEG-coated particles and show good stability of (188)Re/(99m)Tc-SSS labelling.