Synthesis, Biodistribution, and Microsingle Photon Emission Computed Tomography (SPECT) Imaging Study of Technetium-99m Labeled PEGylated Dendrimer Poly(amidoamine) (PAMAM)-Folic Acid Conjugates
Synthesis, Biodistribution, and Microsingle Photon Emission Computed Tomography (SPECT) Imaging Study of Technetium-99m Labeled PEGylated Dendrimer Poly(amidoamine) (PAMAM)-Folic Acid Conjugates
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Technetium-99m 标记的聚乙二醇化树枝状聚合物聚酰胺胺 (PAMAM)-叶酸缀合物的合成、生物分布和微单光子发射计算机断层扫描 (SPECT) 成像研究
DOI：
10.1021/jm901910j
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发表时间：
2010-04-22
影响因子：
7.3
通讯作者：
Shen, Yu-Mei
中科院分区：
文献类型：
--
作者：
Zhang, Yuanqing;Sun, Yanhong;Shen, Yu-Mei
成功合成并放射性标记了三种基于第五代树枝状聚合物 PAMAM 的缀合物。为了研究它们的肿瘤靶向性，分别评估了体外和体内稳定性、细胞摄取、体内生物分布和显微 SPECT 成像。 (99m)Tc 标记的聚乙二醇化树枝状大分子 PAMAM 叶酸缀合物 ((99m)Tc-G5-Ac-pegFA-DTPA) 的缀合物在 KB 癌细胞中表现出比其他两种缀合物更高的摄取，并且在肿瘤区域中积累更多。 KB 细胞的摄取取决于孵育时间。体内生物分布的结果与显微 SPECT 成像获得的数据一致。这些研究表明，PAMAM 树枝状大分子叶酸缀合物的聚乙二醇化可改善肿瘤靶向性。叶酸缀合的树枝状大分子可能被开发为潜在的放射性药物和靶向药物递送系统。
Three conjugates based on dendrimer PAMAM generation five were synthesized and radiolabeled successfully. To investigate their tumor targeting, the in vitro and in vivo stability, cell uptake, in vivo biodistribution, and micro-SPECT imaging were evaluated, respectively. The conjugate of (99m)Tc labeled PEGylated dendrimer PAMAM folic acid conjugate ((99m)Tc-G5-Ac-pegFA-DTPA) shows much higher uptake in KB cancer cells and accumulated more in the tumor area than that of the other two conjugates. The uptake in KB cells depends on the incubation time. The results of in vivo biodistribution agree with the data obtained from micro-SPECT imaging. These studies show that PEGylation of PAMAM dendrimer folic acid conjugate improves the tumor targeting. Folate-conjugated dendrimer maybe developed to be potential radiopharmaceuticals and targeted drug delivery systems.