A single-step kit formulation for the (99m)Tc-labeling of HYNIC-Duramycin.
A single-step kit formulation for the (99m)Tc-labeling of HYNIC-Duramycin.
复制标题
DOI：
10.1016/j.nucmedbio.2012.03.006
复制
发表时间：
2012-10
影响因子：
3.1
通讯作者：
Li Z
中科院分区：
文献类型：
--
作者：
Zhao M;Li Z
99mTc-杜拉霉素是一种独特的与磷脂酰乙醇胺(PE)特异结合的放射性药物。目前的工作是开发一种用于标记HYNIC-杜拉霉素的一步法试剂盒配方。对一系列Tricine/TPPTS配基体系进行了滴定实验，确定了制备高放化纯度和高比活度99mTc-杜拉霉素的最佳配方。使用包覆不同磷脂种类的聚苯乙烯微球对使用试剂盒配方制备的放射性药物的PE结合特异性进行了测试。测定试剂盒在-20℃、室温和37℃下保存后的放化性能，并在静脉注射后3、10、20、60和180分钟测定99mTC-杜拉霉素在健康大鼠体内的生物分布。使用大鼠主动脉弓和大鼠心肌缺血/再灌注模型进行了结合研究，这两种模型代表了生理性和病理性PE外化的情景。当Tricine/TPPTS的比例为10：1时，99mTc-杜拉霉素的产量稳定，放化纯度高(N为90%)，而40：1的比例较高，可生产不完全取代Tricine Coligand的放射性药物。用一步法试剂盒制剂制备的99mTC-杜拉霉素保留了PE结合的特异性。这些试剂盒在长期储存中是稳定的。试剂盒制备的99mTC-杜拉霉素的生物分布与已有研究中的高效液相色谱分离纯化的放射性药物相一致。组织水平的结合研究表明，放射性药物适合于研究在各种生理和病理条件下涉及PE分布和再分布的生物过程。研制了一种用于HYNIC-杜拉霉素99mTc标记的一步法试剂盒配方。该放射性药物具有较高的放射化学纯度和比活度，保留了PE结合活性，易于长期储存，可供体内注射使用。
99mTc-Duramycin is a unique radiopharmaceutical that binds specifically to phosphatidylethanolamine (PE). The current effort is to develop a single-step kit formulation for the 99mTc labeling of HYNIC-Duramycin. A titration series of Tricine/TPPTS coligand systems were tested for an optimal formulation to produce 99mTc-Duramycin with high radiochemical purity and specific activity. The radiopharmaceutical prepared using the kit formulation was tested for PE binding specificity using polystyrene microbeads coated with different phospholipid species. Radiochemical performance of the kits was assessed after storage at –20 °C, room temperature and 37 °C. Biodistribution profile of kit-prepared 99mTc-Duramycin was characterized in healthy rats at 3, 10, 20, 60 and 180 min after intravenous injection. Binding studies were performed using the rat aortic arch and a rat model of myocardial ischemia/reperfusion, which represent scenarios of physiological and pathological PE externalization. A Tricine/TPPTS ratio of 10:1 led to a consistent production of 99mTc-Duramycin with high radiochemical purity (N 90%), whereas a higher ratio at 40:1 produced radiopharmaceuticals with incomplete substitution of Tricine coligand. 99mTc-Duramycin prepared using the single-step kit formulation retained PE-binding specificity. The kits are stable over long-term storage. The biodistribution profile of kit-prepared 99mTc-Duramycin is consistent with HPLC purified radiopharmaceutical from prior studies. Binding studies on a tissue level indicate that the radiopharmaceutical is suitable for studying biological processes that involve PE distribution and redistribution in various physiological and pathological conditions. A single-step kit formulation is developed for 99mTc-labeling of HYNIC-Duramycin. The radiopharmaceutical has high radiochemical purity and specific activity, retained PE binding activities, amiable to long-term storage, and is injection-ready for in vivo applications.
登录
查看更多内容
DOI：
10.1152/ajpheart.1998.274.1.h242
发表时间：
1998-01-01
影响因子：
4.8
作者：
Maulik, N;Kagan, VE;Das, DK
通讯作者：
Das, DK
DOI：
10.1073/pnas.93.23.12867
发表时间：
1996-11-12
影响因子：
11.1
作者：
Emoto, K;Kobayashi, T;Umeda, M
通讯作者：
Umeda, M
影响因子：
4.7
作者：
Edwards, DS;Liu, S;Carroll, TR
通讯作者：
Carroll, TR
影响因子：
2.9
作者：
Li, Zhixin;Wells, Clive W.;Zhao, Ming
通讯作者：
Zhao, Ming
影响因子：
9.3
作者：
Zhao, Ming;Li, Zhixin;Bugenhagen, Scott
通讯作者：
Bugenhagen, Scott