中文摘要：

目的探讨^131I—RGD—BSA—PCL核素纳米载体对非小细胞肺癌荷瘤裸鼠模型SPECT／CT显像效果及其对肿瘤的抑制作用。方法构建纳米脂质体^131I—RGD—BSA—PCL及^131I—BSA—PCL，通过荧光共聚焦显微镜观察该载体在非小细胞肺癌细胞系H460的靶向性结合及细胞摄取情况；采用氯氨T法标记核素纳米载体：流式细胞术观察核素纳米载体对肿瘤细胞的杀伤作用。构建荷瘤裸鼠模型，研究核素纳米载体在荷瘤裸鼠体内的组织分布、肿瘤体积变化及各组荷瘤裸鼠SPECT／CT断层显像。结果给药后1和8h，H460细胞质和细胞核对RGD—BSA—PCL、BSA—PCL两种纳米载体均有明显摄取。Na^131I、^131I-BSA—PCL及^131I—RGD—BSA—PCL对H460细胞的早期凋亡率分别为（33．3±12．5）％、（68．4±8．0）％和（70．5±12．2）％。荷瘤裸鼠体内实验中，给药后24和72h，肿瘤^131I—RGD-BSA-PCL摄取率均高于^131I-BSA—PCL（t=9．53、5．03，P〈0．01）。给药后23d．^131I-RGD-BSA-PCL肿瘤体积抑制最明显（t=126．44，P〈0．01）。SPECT／CT显示，给药后21d，^131I-RGD—BSA—PCL在肿瘤内信号强度明显强于^131I-BSA-PCL。结论^131I标记的纳米脂质体^131I—RGD—BSA—PCL对H460细胞裸鼠移植瘤具有明显的抑瘤作用，且^131I—RGD—BSA—PCL能较长时间停留在肿瘤中。

英文摘要：

Objective To investigate the SPECT/CT imaging of non-small-cell lung carcinoma （NSCLC） mice models and the internal irradiation biological effects and therapeutic effectiveness of nanoliposome ^131I-RGD-BSA-PCL. Methods RGD-BSA-PCL and BSA-PCL were constructed. The target binding and cellular uptake in H460 cell line were observed by fluorescence confoeal microscopy in vitro. The nanoliposome with ^131I were labeled using the Chloramine-T method. Apoptosis analyses was performed using flow cytometry. By construcing tumor xenografts and the SPECT/CT imaging were discussed. Results the biological distribution, change of tumor volume Confocal microscopy revealed signifieant uptake of RGD-BSA-PCL or BSA-PCL in NCI-H460 cell after nanolipsome incubated for 1 and 8 h. The early apoptosis rates of Na^131I, ^131I-BSA-PCL and ^131I-RGD-BSA-PCL were （ 33.3 ± 12. 5 ） %, （ 68.4 ±8. 0） % and （70. 5± 12.2）% , respectively. The tumor uptake levels of ^131I-BSA-PCL were higher than that of ^131I- BSA-PCL （t =9.53, 5.03, P 〈 0. 01 ）. There was a significant difference of tumor volume between the treatment group and the control group, and the tumor volume inhibition was most obvious in the ^131I-RGD- BSA-PCL group on day 23 post-treatment （t = 126.44, P 〈 0. 01 ）. SPECT/CT tomography showed that ^131I-RGD-BSA-PCL and ^131I-BSA-PCL groups had obvious accumulation in the tumor on day 21 posttreatment, and intensity of radiation signal of ^131I-RGD-BSA-PCL group was stronger than that of ^131I-BSA- PCL group. Conclusions Radionuelide therapy using ^131I-RGD-BSA-PCL, which showed excellent targeted cell killing and suppressed tumor growth, exhibited favorable intracellular retention of ^131I.