期刊
NUCLEAR MEDICINE AND BIOLOGY
卷 36, 期 5, 页码 515-524出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.nucmedbio.2009.02.004
关键词
Rhenium-186; Doxil; Biodistribution; Pharmacokinetics; SPECT/CT; Liposome; Nanoparticle
资金
- National Institutes of Health [5P30CA054174]
The purpose of this study was to determine the feasibility of radiolabeling liposomal doxorubicin (Doxil) for cancer chemoradionuclide therapy by directly loading the therapeutic radionuclide rhenium-186 (Re-186) into the liposome interior. The pharmacokinetics, imaging and biodistribution of [Re-186]Doxil (555 MBq/kg) and control [Re-186]polyethylene glycol (PEG) liposomes (555 MBq/kg) were determined after intravenous administration in a head and neck cancer xenograft model in nude rats. [Re-186]Doxil and [Re-186]PEG liposomes were radiolabeled using [Re-186]N,N-bis(2-mercaptoethyl)-N',N'-diethylethylenediamine. Re-186 labeling efficiency was 76.1 +/- 8.3% with Doxil. The in vitro serum stability of [Re-186]Doxil at 37 degrees C was 38.06 +/- 12.13% at 24 h. Pharmacokinetic studies revealed that [Re-186]Doxil had a two-phase blood clearance with half clearance times of 0.8 and 28.2 h. Images acquired over 120 h showed that [Re-186]Doxil had slow blood clearance, low liver accumulation and increasing spleen accumulation. The biodistribution study at 120 h indicated that the percentage of injected dose (%ID) in the blood and tumor for [Re-186]Doxil was 20-fold higher than that of [Re-186]PEG liposomes. The %ID values in the kidney and liver were not significantly different between [Re-186]Doxil and [Re-186]PEG liposomes. These results suggest that the long circulation and prolonged bioavailability of [Re-186]Doxil could potentially deliver high concentrations of both doxorubicin and Re-186 to tumor when encapsulated in the same liposome vehicle. (C) 2009 Elsevier Inc. All rights reserved.
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