Abstract: Objective To investigate a new biologic-superparamagnetic nanoparticles's characteristics of immunological activity, biological distributing in vivo, targeting and inhibiting tumoreffect. Methods The experimental group ¹⁸⁸Re-Hepama-1-superparamagnetic nanoparticles, and control groups, including ¹⁸⁸ReO₄^-, ¹⁸⁸Re-Hepama-1, and ¹⁸⁸Re-superparamagnetic nanoparticles, were set up. The distributions were measured after injection 4 h and 24 h by caudal vein of Kuming mice. The magnetic targeting experiments in vivo were done with and without magnetic field in liver after injection in New Zealand rabbit. The inhibiting tumor effect on hepatic cancer cell lines SMMC-7721 of the above four ¹⁸⁸Re labeled products were measured by mono nuclear cell direct cytotoxicity assay method. Results After injection 4 h and 24 h by vein, the liver taking was highest in group ¹⁸⁸Re-Hepama-1-superparamagnetic nanoparticles. The radiative activity in liver in magnetism zoo was higher than in non magnetism zoo in ¹⁸⁸Re-Hepama-1-superparamagnetic nanoparticles after applying magnetic field in left lobe of liver, and the ratio of in magnetism zoo to non magnetism zoo was 1.87. And the half effective inhibition radioactive concentrations (IC₅₀) in ¹⁸⁸Re-Hepama-1-superparamagnetic nanoparticles was one forth of ¹⁸⁸ReO₄^-. Conclusion ¹⁸⁸Re-Hepama-1-superparamagnetic nanoparticles showed its fine stability in intro, good immunological activity and significant liver target.