Cheng Yongjun, Zhu Jingyi, Zhao Lingzhou, Xiong Zhijuan, Tang Yueqin, Liu Changcun, Guo Lilei, Qiao Wenli, Shi Xiangyang, Zhao Jinhua
Department of Nuclear Medicine, Shanghai General Hospital, School of Medicine, Shanghai Jiaotong University, Shanghai 200080, People's Republic of China.
State Key Laboratory for Modification of Chemical Fibers & Polymer Materials, College of Materials Science & Engineering, Donghua University, Shanghai 201620, People's Republic of China.
Nanomedicine (Lond). 2016 May;11(10):1253-66. doi: 10.2217/nnm-2016-0001. Epub 2016 Mar 4.
The poly(amidoamine) dendrimers modified with Buthus martensii Karsch chlorotoxin (BmK CT) were developed as a (131)I delivery system for glioma-targeted imaging and therapy.
MATERIALS & METHODS: Dendrimers before and after labeling (131)I were synthetized and their physicochemical properties were tested. The targeting and therapeutic efficacy of (131)I-G5.NHAc-HPAO-(PEG-BmK CT)-(mPEG) dendrimer against glioma was evaluated in vitro and in vivo.
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. (131)I-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.
(131)I-G5.NHAc-HPAO-(PEG-BmK CT)-(mPEG) complex is a promising multifunctional nanoplatform for glioma-specific nuclear imaging and radiotherapy.
研发用东亚钳蝎氯毒素（BmK CT）修饰的聚酰胺-胺树枝状大分子作为用于胶质瘤靶向成像和治疗的¹³¹I递送系统。
合成了标记¹³¹I前后的树枝状大分子，并测试了其理化性质。在体外和体内评估了¹³¹I-G5.NHAc-HPAO-(PEG-BmK CT)-(mPEG)树枝状大分子对胶质瘤的靶向性和治疗效果。
所有树枝状大分子在不同条件下均稳定。BmK CT修饰增加了树枝状大分子在C6胶质瘤细胞中的细胞摄取，但在正常RLE-6TN细胞中未增加。¹³¹I-G5.NHAc-HPAO-(PEG-BmK CT)-(mPEG)树枝状大分子放射化学纯，可用于胶质瘤靶向单光子发射计算机断层扫描（SPECT）成像和放射治疗。
¹³¹I-G5.NHAc-HPAO-(PEG-BmK CT)-(mPEG)复合物是一种有前景的用于胶质瘤特异性核成像和放射治疗的多功能纳米平台。
