(68)Ga-NOTA-CHSg and (99m)Tc-CHSg Labeled Microspheres for Lung Perfusion and Liver Radiomicrospheres Therapy Planning.
(68)Ga-NOTA-CHSg and (99m)Tc-CHSg Labeled Microspheres for Lung Perfusion and Liver Radiomicrospheres Therapy Planning.
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DOI：
10.1155/2013/279872
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发表时间：
2013
期刊：
影响因子：
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通讯作者：
McGoron AJ
中科院分区：
文献类型：
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作者：
Amor-Coarasa A;Milera A;Carvajal D;Gulec S;Leichner J;McGoron AJ
PET 和 SPECT 肺灌注和放射性微球治疗计划需要快速生物降解（12 小时 < 半衰期 < 48 小时）放射性标记微球。采用乳液法制备了具有可生物降解的壳聚糖二醇（CHSg）的30.1±4.8μm尺寸范围的微球。在灌注 PET 和 SPECT 研究中，用 99mTc 或 68Ga 来表征和标记微球，作为 MAA 的替代品。用 p-SCN-Bn-NOTA 对 CHSg 微球进行表面修饰，以提高 68Ga 的体内稳定性。 99mTc 直接标记到 CHSg 微球上。评估了标记产量和体外放射化学稳定性。体外 CHSg 微球在猪血液中的降解半衰期约为 24 小时。将标记的微球注射到 Sprague Dawley 大鼠体内，并在 2 小时和 4 小时后测定生物分布。 99mTc-CHSg 和 68Ga-NOTA-CHSg 注射后均迅速分配到肺部。 99mTc-CHSg 显示 2 小时和 4 小时后分别有 91.6 ± 6.5% 和 83.2 ± 4.1% 的衰变校正注射活性残留在肺部。对于获得的 68Ga-NOTA-CHSg 微球，肺分配非常高，2 小时和 4 小时后分别为 98.9 ± 0.2% 和 95.6 ± 0.9%。添加 p-SCN-Bn-NOTA 可充当辐射防护剂，消除从肺部释放到膀胱的 68Ga 活性，从而保护其他器官。
Fast biodegradable (12 h < half-life < 48 h) radioactive labeled microspheres are needed for PET and SPECT lung perfusion and radiomicrosphere therapy planning. An emulsion method was used to create 30.1 ±4.8 μm size range microspheres with biodegradable Chitosan glycol (CHSg). Microspheres were characterized and labeled with 99mTc or 68Ga as an alternative to MAA in perfusion PET and SPECT studies. Surface decoration of CHSg microspheres with p-SCN-Bn-NOTA was performed to increase 68Ga in vivo stability. 99mTc was labeled directly to the CHSg microspheres. Labeling yield and in vitro radiochemical stability were evaluated. In vitro CHSg microsphere degradation half-life was ~24 hours in porcine blood. Labeled microspheres were injected into Sprague Dawley rats and biodistribution was determined after 2 and 4 hours. Both 99mTc-CHSg and 68Ga-NOTA-CHSg were quickly allocated in the lungs after injection. 99mTc-CHSg showed 91.6 ± 6.5% and 83.2 ± 4.1% of the decay corrected injected activity remaining in the lungs after 2 and 4 hours, respectively. For the obtained 68Ga-NOTA-CHSg microspheres, lung allocation was very high with 98.9 ± 0.2% and 95.6 ± 0.9% after 2 and 4 hours, respectively. The addition of p-SCN-Bn-NOTA acts as a radioprotectant eliminating the released 68Ga activity from the lungs to the bladder protecting the other organs.