- 作者：Hsin-Ell Wang ; Hung-Man Yu ; Yi-Ching Lu ; Ning-Ning Heish ; Yun-Long Tseng ; Kuang-Liang Huang ; Kuo-Tang Chuang ; Chin-Hsiung Chen ; Jeng-Jong Hwang ; Wuu-Jyh Lin ; et al.
- 关键词：Radiolabeled pegylated liposomes ; Targeted radionuclide therapy ; Dosimetry ; Lutetium-177 ; Indium-111
- 刊名：Nuclear Instruments and Methods in Physics Research Section A ; Accelerators ; Spectrometers ; Detectors and Associated Equipment
- 出版年：2006
- 期刊代码：41_01689002
- 类别：ph
- 出版时间：20 December 2006
- 卷：569
- 期：2
- 页码：533-537
- 文件大小：256 K
Methods
The DTPA/PEG-liposomes were synthesized with a medium size of 110 nm, conjugated with 111In/177Lu-(oxine)3 to afford 111In/177Lu-liposome. The stability of 111In/177Lu-liposome in serum was investigated. The biodistribution, scintigraphic imaging and pharmacokinetics of 111In/177Lu-liposomes after intravenous(i.v.) injection into C-26 tumor-bearing BALB/cByJ mice were studied. Radiation dose was estimated by MIRD-III program.
Results
The incorporation efficiency of 111In/177Lu into liposomes was 95%. After incubation at 37 °C for 72 h in serum, more than 83%of radioactivity was still retained in the intact 111In/177Lu-liposomes. The biodistribution of 111In-liposomes showed that the radioactivity in the blood decreased from 23.14±8.16%ID/g at 1 h to 0.02±0.00%ID/g at 72 h post-injection (p.i.), while reaching its maximum accumulation in tumors at 48 h p.i., with half-life in blood of 10.2 h. The results were supported by that of 177Lu-liposomes. Scintigraphic imaging with 111In-liposomes showed unambiguous tumor images at 48 h p.i. Dose estimation showed that the absorbed dose in tumor from 177Lu-liposomes was 5.74×10−5 Gy/MBq.
Conclusions
This study provides an in vivo characterization and dosimetric evaluation for the use of liposome systems as carriers in targeted radionuclide therapy. The results suggest that adequate tumor targeting as well as dose delivered to tumors could be achieved by the use of radionuclide targeted liposomes.