177Lu-DOTA-MHI 148多模态显像剂在乳腺癌MCF-7鼠瘤模型的体内分布及活体成像研究

In vivo Distribution and in vivo Imaging of 177Lu-DOTA-MHI 148 Multimodal Imaging Agent in Breast Cancer MCF-7 Mouse Tumor Model

目的以DOTA-MHI 148为靶向肿瘤细胞的探针,用放射性核素镥(177Lu)标记DOTA-MHI 148合成双模态分子探针,探讨其在乳腺癌MCF-7裸鼠模型中的生物分布及显像情况。材料与方法以177Lu标记DOTA-MHI 148,使用高效液相色谱法测定标记物的标记率及室温稳定性。研究该分子探针在乳腺癌荷瘤裸鼠模型中的生物分布及γ闪烁成像和近红外荧光成像情况。结果177Lu-DOTA-MHI 148在1 h时的标记率为(97.83±0.62)%,室温放置24 h后标记率为(95.75±0.56)%。生物分布结果显示,肿瘤内标记物的分布随时间增加而逐渐增高,在48 h分布达到最高,为(4.69±2.28)%ID/g,且肿瘤/肌肉比值达到最高,为40.53±16.09。成像结果显示,在48 h时肿瘤显影效果最佳。结论成功制备多模态分子探针177Lu-DOTA-MHI 148,该分子探针具有较好的室温稳定性。体内生物分布及γ闪烁成像、近红外荧光成像结果显示177Lu-DOTA-MHI 148具有良好的肿瘤靶向性,证实177Lu-DOTA-MHI 148在肿瘤的诊断及治疗中具有潜在的临床应用价值。

Purpose Using DOTA-MHI 148 as a probe targeting tumor cells,lutetium(177Lu)labeled with DOTA-MHI 148,and synthesized a bimodal molecular probe to investigate the biodistribution and imaging of MCF-7 in nude mice.Materials and Methods DOTA-MHI 148 was labeled with 177Lu,the labeling rate and room temperature stability were determined by HPLC.The biodistribution of the probe in the nude mice model of breast cancer and the situation ofγ-scintigraphy and near infrared fluorescence imaging were studied.Results At one hour,the labeling rate of 177Lu-DOTA-MHI 148 was(97.83±0.62)%.After 24 hours at room temperature,the labeling rate was(95.75±0.56)%.The results of biodistribution showed that the distribution of markers increased with time,and reached the highest level(4.69±2.28)%ID/g at 48 hours,and the ratio of tumor to muscle was the highest of 40.53±16.09.The imaging results showed that the tumor imaging effect was best at 48 hours.Conclusion 177Lu-DOTA-MHI 148,a multimode molecular probe,is successfully prepared.The probe has good room temperature stability.The results of biodistribution,γscintigraphy and near infrared fluorescence imaging shows that 177Lu-DOTA-MHI 148 has good tumor targeting.It is proved that 177Lu-DOTA-MHI 148 has potential clinical application value in the diagnosis and treatment of tumor.