本研究以具有优良生物学性能的近红外核交联聚合胶束纳米粒子（NIRF-CCPM）为载体，将具有肿瘤靶向性的多肽RGD（精氨酸-甘氨酸-天冬氨酸）与该纳米粒子偶联，并通过放射性核素¹¹¹In进行标记，放射性标记过程中，标记率96%，放化纯度大于99%. ¹¹¹In-CCPM-RGD分子探针表现出良好的放射标记/光学性质. 体外稳定性研究表明，25 ℃条件下其在5%小牛血清缓冲液中静置72 h，依然保持有90%的稳定性. 同时采用核医学/光学显像两种影像手段评价了该双模态分子探针在U87肿瘤模型裸鼠体内的代谢情况：在静脉注射11.1 MBq ¹¹¹In-CCPM-RGD纳米粒子24 h、72 h进行SPECT/CT的显像，其在肿瘤部位表现出特异性的浓集. 同时，其在NIRF的显像中表明相应肿瘤区域出现特异性富集. ¹¹¹In-CCPM-RGD纳米粒子的设计、合成及初步生物学评价说明其同时兼具光学和核医学显像功能，是性能优良的新型双模态纳米分子探针，能够帮助提高肿瘤的诊断效能，为建立光学/核医学用于肿瘤靶向双模式成像奠定理论基础.

The multi-modality probes are essential for multi-modality imaging. Dual labeled imaging probes allow the same target to be evaluated with two different modalities. Based on the structure of c-RGD peptide motif, some examples of multimodality agents have been reported in design of RGD for α_vβ₃ intergin positive tumor imaging. The aim of this study was to develop a dual-labeled nanoparticles for both single photon emission computed tomography (SPECT) and near-infrared fluorescence (NIRF) imaging of α_vβ₃. In this paper, c-RGD was conjugated to near-infrared fluorescence fluorophores (Cy7) entrapped polyethylene glycol-coated, core-crosslinked polymeric micelles (NIRF-CCPM) labeled with a radioisotope indium 111. The labeling efficiency was over 96%, the radio chemical purity was over 99% after purification. The in vitro stability tests were presented in 5% bull serum albumin (BSA) for 72 h at 25 ℃. Less than 10% ¹¹¹In dissociation was detected by Radio-Thin-Layer Chromatography. ¹¹¹In-CCPM-RGD seems to be a promising candidate for dual optical and nuclear imaging applications in tumor detection. Its structure was fully characterized. Serial SPECT imaging of human glioma U87 tumor-bearing nude mice revealed that tumor uptake of ¹¹¹In-CCPM-RGD got a substantial growth from 24 h to 72 h after post-injection of 11.1 MBq nanoparticles, corroborated by in vivo NIRF imaging. Tumor uptake as measured by in vivo NIRF imaging by region of interest (ROI) with the unit of average radiant efficiency. The ROI of tumor NIRF imaging were 4.81×10⁷ and 6.91×10⁷ [p/sec/cm²/sr]/[μW/cm²] at 24 h, 72 h respectively. The in vivo SPECT imaging was general concordance with NIRF imaging. The combination of these nuclear and NIRF imaging technologies will significantly improve the accuracy in tumor diagnosis. The persistent, excellent, and α_vβ₃-specific uptake of ¹¹¹In-CCPM-RGD in the tumor, observed by both SPECT and NIRF imaging, warrants further investigation and future clinical translation of such nanoparticles-based imaging agents.