131I-labeled multifunctional dendrimers modified with BmK CT for targeted SPECT imaging and radiotherapy of gliomas
131I-labeled multifunctional dendrimers modified with BmK CT for targeted SPECT imaging and radiotherapy of gliomas
复制标题
(131)I 标记的多功能树枝状大分子经 BmK CT 修饰，用于胶质瘤的靶向 SPECT 成像和放射治疗。
DOI：
10.2217/nnm-2016-0001
复制
发表时间：
2016-01-01
期刊：
影响因子：
5.5
通讯作者：
Zhao, Jinhua
中科院分区：
文献类型：
--
作者：
Cheng, Yongjun;Zhu, Jingyi;Zhao, Jinhua
目的：利用马氏Buthus martensii Karsch chlorotoxin （BmK CT）修饰的聚胺胺树状大分子（poly(amidoamine) dendrimers）作为脑胶质瘤靶向成像和治疗的I-131递送系统。材料与方法：合成标记I-131前后的树状大分子，并对其理化性质进行测试。I-131-G5的靶向性及治疗效果。在体外和体内评价nacc - hpao -(PEG-BmK CT)-(mPEG)树突状物对胶质瘤的作用。结果：所有树状大分子在不同条件下均稳定。BmK CT修饰增加了C6胶质瘤细胞对树突分子的摄取，而正常RLE-6TN细胞则没有。i - 131 - g5。nacc - hpao -(PEG-BmK CT)-(mPEG)树突状物放射化学纯度高，可用于胶质瘤靶向单光子发射CT （SPECT）成像和放疗。结论:i - 131 - g5。nacc - hpao -(PEG-BmK CT)-(mPEG)复合物是一种很有前途的用于胶质瘤特异性核成像和放疗的多功能纳米平台。
Aim: The poly(amidoamine) dendrimers modified with Buthus martensii Karsch chlorotoxin (BmK CT) were developed as a I-131 delivery system for glioma-targeted imaging and therapy. Materials & methods: Dendrimers before and after labeling I-131 were synthetized and their physicochemical properties were tested. The targeting and therapeutic efficacy of I-131-G5.NHAc-HPAO-(PEG-BmK CT)-(mPEG) dendrimer against glioma was evaluated in vitro and in vivo. Results: All the dendrimers were stable under different conditions. BmK CT modification increased the cellular uptake of dendrimers in C6 glioma cells, but not in the normal RLE-6TN cells. I-131-G5.NHAc-HPAO-(PEG-BmK CT)-(mPEG) dendrimer was radiochemically pure and could be applied in glioma-targeting single-photon emission CT (SPECT) imaging and radiotherapy. Conclusion: I-131-G5.NHAc-HPAO-(PEG-BmK CT)-(mPEG) complex is a promising multifunctional nanoplatform for glioma-specific nuclear imaging and radiotherapy.