188Re-Herceptin-磁性纳米微粒的体外抗肿瘤作用

目的探讨^188Re—Herceptin-磁性纳米微粒在外置磁场下对HER-2／neu癌基因高表达的SKBR-3乳腺癌细胞的靶向结合性及抗癌作用。方法采用戊二醛交联法使人源性单克隆抗体Her—ceptin与磁性纳米微粒交联，用直接标记法制备^188Re—Herceptin及^188Re—Herceptin-磁性纳米微粒，用羰基铼标记法制备^188Re-磁性纳米微粒。肿瘤细胞体外抑制实验设4个组：^188Re—Herceptin-磁性纳米微粒组、^188Re—Herceptin组、^188Re-磁性纳米微粒组和^188ReO4^-组，各组均设3．7×10^4、18．5×10^4、37×10^4、55．5×10^4、74×10^4Bq／ml5个放射性剂量级别；另设生理盐水对照组。采用四甲基偶氮唑蓝（MTT）法测定各组的抑瘤效应，计算相对抑制率，采用半数抑制放射性浓度（IC50）对各组抑瘤作用进行比较和评价。结果^188Re—Herceptin-磁性纳米微粒和^188Re—Herceptin组对SKBR-3细胞均有较强杀伤作用，且呈剂量依赖性；而^188Re-磁性纳米微粒和^188Re04组的杀伤作用较弱0188Re—Herceptin-磁性纳米微粒组的IC50（53．1×10^4Bq／L）明显低于^188Re—Herceptin组（76．1×10^4Bq／L）；^188Re一磁性纳米微粒组和^188ReO4组的IC50分别为169×10^4和175×10^4Bq／L，明显高于前2组。结论^188Re—Herceptin-磁性纳米微粒和^188Re—Herceptin均可明显抑制体外培养的SKBR-3乳腺癌细胞增殖，且前者的抑制作用较后者强。     

[188Re(CO)3(H2O)3]+间接标记免疫磁性纳米微粒的实验研究

目的探讨标记单克隆抗体磁性纳米微粒的实验条件。方法以[二（2-吡啶甲基）-氨基]-乙酸（PADA）作为双功能螯合剂，将[^188Re（CO）3（H2O）3]^＋间接标记到耦联了单克隆抗体的磁性纳米微粒。结果[^188Re（CO）3（H2O）3]^＋间接标记免疫磁性纳米微粒的标记率大于80％，在小牛血清和生理盐水中48h后稳定性仍能保持在90％以上。结论使用PADA作为双功能螯合剂，[^188Re（CO）3（H2O）3]^＋间接标记免疫磁性纳米微粒的标记率高，稳定性好，适于进一步体内研究。     

抗人肝癌188Re-免疫磁性纳米微粒的生物学分布和肿瘤细胞抑制实验

目的探讨抗人肝癌188Re-免疫(Hepama-1)磁性纳米微粒免疫学活性、体内生物学分布、肝靶向性及抑瘤作用。方法对比188ReO4-、188Re-Hepama-1、188Re-磁性纳米微粒,研究尾静脉注射188Re-免疫磁性纳米微粒后4h、24h在昆明小鼠体内的分布情况;在肝区外加磁场及无磁场状态下,研究新西兰大白兔体内的肝磁靶向性;采用溴化四甲基唑法,研究4种188Re标记物对肝癌细胞株SMMC-7721的抑制效果。结果188Re-免疫磁性纳米微粒在肝内摄取量最大;在磁区肝组织放射活性较非磁区肝组织明显增加,二者的放射活性比值为1.87;对肝癌细胞株SMMC-7721半数抑制放射性活度仅为188ReO4-的1/4左右。结论188Re-磁性纳米微粒具有良好的磁感应性能、免疫活性及明显的肝靶向性。     

188 Re直接法标记生长抑素类似物RC-160及其体内分布研究

目的 探讨^188RE直接法标记生长抑素类似物RC－160的方法及观察其在小鼠体内的生物学分布。方法 酒石酸亚锡直接还原法进行RC－160的^188Re标记，标记完成后加入抗坏血酸以防标记产物的再氧化。硅胶纸层析测定放化纯，并行小鼠体内分布实验。结果 ^188Re－RC－160放化纯为96．2％，游离^188Re为0．8％，放射性胶体为3．0％。加抗坏血酸组在标记后24h放化纯为85％，对照组为50％。注射后0．5－1．0h血液中放射性下降了87．2％，肾脏无明显浓集，标记物24h内由消化系统排出体外。结论 ^188Re直接法标记RC－160放化纯高，方法简便，抗坏血酸的加入增加了标记物的稳定性。^188Re－RC－160在小鼠体现血液清除较快，经消化系统排除。     

胶体铼及其应用

胶体铼按所标核素的不同分为^188Re标记的胶体铼和其他核素标记的胶体铼。在放射性关节滑膜切除术中，用^188Re标记的硫化胶体铼是一种有效的治疗手段，对于荷瘤(如黑色素瘤、肝癌等)小鼠也有一定的治疗效果。淋巴显像中^99Tc^m标记的胶体铼是前哨淋巴结显像中常用的一种显像剂。     

188Re-DTPA-DG的制备和荷瘤裸鼠实验研究

目的建立^188Re标记DTPA-脱氧葡萄糖（DG）的方法，观察其在荷瘤裸鼠体内分布和治疗效果。方法DTPA—DG的^188Re标记体系有氯化亚锡、葡萄糖酸钠，pH值5．5，反应体系温度为37％，反应3h，用纸层析法以生理盐水和丙酮作展开剂，测定标记物的放化纯及其在体外的稳定性。将标记物经荷乳腺癌MCF-7裸鼠尾静脉注射，于注射后1，4，8，12，24h显像。经尾静脉注射0．1ml 92．5GBq／L的^188Re—DTPA—DG，21d后观察疗效。结果^188Re—DTPA—DG的放化纯可达到95．0％。^188Re—DTPA—DG荷瘤裸鼠显像示肿瘤组织摄取高，病灶／健侧后肢对应部位放射性计数（T／NT）比值在12和24h分别为5．9和7．8。^188Re-DTPA-DG组裸鼠治疗21d后肿瘤体积[（823．6±50．58）mm^3]明显比生理盐水组[（1162．7±73．08）mm^3]小，2组间差异有统计学意义（P〈0．01），抑瘤率为29．2％。结论^188Re—DTPA—DG经荷瘤裸鼠尾静脉注射后可被肿瘤组织高选择性摄取，其对肿瘤生长抑制作用明显，可能成为肿瘤内照射治疗药物。     

荷人结肠癌裸鼠瘤内注射^188Re—C50放射免疫治疗实验研究

目的 评价直接法^188Re标记抗CEA单克隆抗体C50和荷人结肠癌裸鼠瘤内注射^188Re－C50放射免疫治疗效果。方法 室温条件下,取4mg维生素C还原C50,0．5h后加入氯化亚锡0．2mL和新鲜淋洗的^188Re370－740MBq,混匀后反应2h以完成整个标记过程。荷人结肠癌裸鼠瘤内分别注射不同剂量的^188Re－C50,观察其治疗作用,并与瘤内注射生理盐水组和^188Re淋洗液组进行比较。结果 标记单抗经放化纯检测,标记液中游离^188Re和胶体^188Re分别少于5％和10％。与对照组比较,瘤内注射14．06MBq以上的标记单抗,其肿生长体积或质量受到明显抑制,甚至体积缩小。结论 直接法^188Re标记C50取得预期结果;瘤内注射^188Re－C50对肿瘤生长有明显的治疗作用。     

载药磁性纳米微粒靶向治疗肿瘤研究进展

载药磁性纳米微粒是将药物、生物活性物质或治疗用放射性核素等包裹于磁性纳米微粒内或吸附、连接于磁性纳米微粒表面，或混合、溶解于材料基质中而构成，其大小为纳米级。在足够强的外加磁场作用下，其在体内定向移动、定向浓集，从而达到提高治疗效果、降低毒副作用的目的。     

99Tcm-Cl2MDP-明胶微粒的制备及其肝脾靶向性研究

目的 研究粒径300-500nm、表面带正电荷的明胶微粒对二氯亚甲基二膦酸盐(Cl2MDP)的包封技术，并观察明胶微粒和载药明胶微粒在SD大鼠体内的分布。方法 通过静电吸附将Cl2MDP连接到明胶微粒表面完成药物包封。用^99Tc^m标记，进行SD大鼠生物学分布实验和显像，观察明胶微粒和Cl2MDP-明胶微粒的组织靶向特征。结果 通过静电吸附法可将Cl2MDP连接到明胶微粒表面，其药物包封效率约为20%，最大载药量达6mg/mg明胶微粒；生物学分布实验和放射性核素显像示其具有较好的肝脾靶向性，可将Cl2MDP定向输送到巨噬细胞，肝脾的摄取超过注射量用60%。结论 该明胶微粒具有良好的肝脾网状内皮系统靶向性，是较理想的肝脾巨噬细胞为作用靶点的药物靶向输送载体；明胶微粒通过静电吸附的方法包封Cl2MDP简便要行，具有较高的药物包封效率和载药量。     

载药肿瘤微血管栓塞颗粒制备及其抗肿瘤作用初探

目的 制备加载化疗药物的纳米微粒,研究其性质及体外释药特点,探讨体外对人原代肝癌细胞的毒性作用,为用于临床肿瘤微血管介入栓塞提供理论依据.方法 以盐酸吉西他滨-复方甘草酸苷共聚物为药物载体,加载化疗药物多柔比星制备载药纳米微粒.扫描电镜观察微粒形态,纳米粒度电位仪检测微粒粒径分布及电位,高效液相色谱法计算载药率及包封率,透析袋扩散法作体外释放动力学试验,体外考察纳米药物稳定性及释药性能.CCK-8法检测纳米药物在体外对人原代肝癌细胞的毒性作用.结果 本法制备的载药纳米微粒外观呈圆球形,平均粒径(62.83±5.19) nm,平均电位-17.9 mV;载药率、包封率分别为3.16％、66.27％;有良好的缓释特性,对人原代肝癌细胞生长有明显抑制作用.结论 本法制备的载药纳米微粒具有较好的药物缓释性及抗肿瘤效应,是一种具有良好应用前景的抗肿瘤纳米药物.     

Radiolabeling morpholinos with 90Y, 111In, 188Re and 99mTc

This laboratory is investigating morpholinos (MORF), a DNA analogue, for radiopharmaceutical applications. While we routinely radiolabel with (99m)Tc, we have now labeled MORFs with (111)In, (188)Re and (90)Y in anticipation of therapeutic studies. METHODS: A 25 mer MORF with a primary amine on the 3' equivalent end attached via a 10 member linker was conjugated with an isothiocyanate backbone derivative of DOTA (for labeling with (111)In and (90)Y) and with NHS-MAG(3) (for labeling with (188)Re and (99m)Tc). The in vitro stability of labeled MORFs were investigated and biodistribution was carried out in normal mice. RESULTS: As evident by size exclusion HPLC, ITLC and Sep-Pak analysis, all four radiolabeled MORFs were successfully radiolabeled. In each case, the labeled MORFs showed one sharp peak in HPLC that shifted completely to earlier retention times following addition of a polymer conjugated with the complementary MORF. In saline at room temperature and in 37 degrees C serum, the radioactivity profile of (111)In, (188)Re and (99m)Tc was unchanged over 48 h while over the same period, the (90)Y profile showed a pronounced lower molecular weight peak which did not shift and was shown to be most probably due to (90)Y-DOTA resulting from radiolysis. In addition, the recovery of (188)Re on HPLC decreased as samples aged probably due to oxidation to perrhenate which was retained by the HPLC column. The biodistributions at 1, 3 and 6 h in normal mice showed no important differences among all four labels with the exception that levels of radioactivity in stomach and thyroid were higher in the case of (188)Re due to in vivo oxidation of the radiolabel to perrhenate. CONCLUSIONS: When radiolabeled with DOTA, (90)Y-labeled MORF showed increased instabilities relative to that of (111)In and when radiolabeled with MAG(3), (188)Re showed in vitro and in vivo instabilities compared to (99m)Tc, but all labels were still largely intact after 48 h in saline or serum. Possibly because of the rapid clearance of MORFs, no important differences in biodistribution among (90)Y, (111)In and (99m)Tc labels were evident in normal mice. These strategies for labeling MORF with (90)Y and (188)Re therefore appear to be suitable for therapeutic applications although both show some evidence of instabilities.     

Radiolabelling morpholinos with 188Re tricarbonyl provides improved in vitro and in vivo stability to re-oxidation

BACKGROUND: For pretargeting and other nuclear medicine applications, it may eventually be useful to radiolabel phosphodiamidate morpholinos (MORFs) with therapeutic radionuclides such as 188Re. However, by preparing 188Re-MORFs labelled conventionally with MAG3 as chelator, we have observed unacceptable levels of oxidation to perrhenate in vitro and in vivo in mice. OBJECTIVE: To improve upon stability, tricarbonyl labelling was considered since tricarbonyl complexes are thought to stabilize metals in low oxidation states. METHODS: An amine derivatized 25 mer MORF was conjugated with either NHS-MAG3 or NHS-Hynic. The MAG3 conjugated MORF was radiolabelled conventionally with 188Re while the Hynic conjugated MORF was radiolabelled through its tricarbonyl intermediate. Using a commercial kit modified with additional reducing agent over that required for the preparation of the 99mTc tricarbonyl complex [99mTc(CO)3(H2O)3]+, we demonstrated that the equivalent 188Re tricarbonyl, [188Re(CO)3(H2O)3]+, could be prepared. Simple incubation at elevated temperatures with the Hynic conjugated MORF then provided 188Re-(CO)3-Hynic-MORF. Confirmation was achieved by a shift assay using a complementary MORF conjugated polymer and size exclusion HPLC. To evaluate the relative stability of the tricarbonyl labelled MORF compared to the MAG3 labelled MORF in vitro, the radiolabelled MORFs were incubated in phosphate buffer and the presence of perrhenate measured periodically by strip chromatography. Stability in vivo was evaluated by biodistribution studies in normal mice. RESULTS: The overall yields for tricarbonyl intermediates averaged greater than 90% for 99mTc and 60-80% for 188Re. Yields following subsequent labelling to Hynic-MORF were about 60-80% for 99mTc and 15-20% for 188Re. The in vitro stability results in phosphate buffer showed that 188Re-MAG3-MORF was fully oxidized by 48 h while 188Re-(CO)3-Hynic-MORF was less than 20% oxidized at that time. Similarly, the 188Re-(CO)3-Hynic-MORF biodistribution in normal mice showed lower radioactivity level in stomach, intestines and thyroid compared with 188Re-MAG3-MORF. CONCLUSION: 188Re-tricarbonyl labelling of Hynic conjugated MORFs may be considerably more stable to oxidation than the MAG3 labelled MORFs and therefore more suitable for radiotherapy trials.     

Radiolabeling of dextran with rhenium-188.

This study describes a method for the radiolabeling of dextran with rhenium-188 (188Re). In nuclear oncology 188Re is very useful for therapeutic applications. Its nuclear characteristics allow radiotherapy and in situ monitoring of tumor uptake as well as dosimetry calculations. Consequently new compounds with this radiolabel are of general interest. Dextran was oxidized with sodium periodate yielding reactive aldehyde groups and subsequently reacted with cysteine. The linkage was stabilized by reducing the Schiff bases with sodium cyanoborohydride. The conjugate was then radiolabeled with 188Re by using 188Re-gluconate as the transchelator, labeling the free thiols. Synthesis and radiolabeling were done in the absence of oxygen. The labeling efficiency was 60-70% and the radiochemical purity > 95%. The in vitro stability study, using "cysteine challenge" demonstrated that 50% of the radiolabel was transcomplexed to the 100 mM cysteine solution (after 1 h incubation at 37 degrees C). However, at physiologic conditions and presence of an antioxidant good stability was achieved. The 188Re labeled dextran presented in this study provides a template with therapeutic and diagnostic potential in nuclear oncology, either alone for local treatment or as a backbone in a tumor specific conjugate for systemic treatment.     

99mTc/188Re-labelled lipid nanocapsules as promising radiotracers for imaging and therapy: formulation and biodistribution

Purpose This study focusses on a promising carrier system for imaging and therapeutic purposes using lipid nanocapsules. To assess their potential for clinical use, we labelled nanocapsules with ^99mTc and ¹⁸⁸Re and analysed some kinetic biodistribution parameters after intravenous injection in rats. Methods Lipophilic complexes [^99mTc/¹⁸⁸Re(S₃CPh)₂(S₂CPh)] (^99mTc/¹⁸⁸Re-SSS) were encapsulated within the nanoparticles during their manufacture with quantitative yield and satisfactory radiochemical purity. Rats were injected intravenously with 3.7 MBq ^99mTc/¹⁸⁸Re-labelled nanocapsules and sacrificed at 5, 15 and 30 min and 1, 2, 4, 8, 12, 16, 20 and 24 h. Results Dynamic scintigraphic acquisitions showed predominant hepatic uptake, and ex vivo counting indicated a long circulation time of labelled nanocapsules, with a half-life of 21±1 min for ^99mTc and 22±2 min for ¹⁸⁸Re. Very weak urinary elimination was observed, indicating good stability of ^99mTc and ¹⁸⁸Re labelling. Conclusion ^99mTc/¹⁸⁸Re-SSS nanocapsules can be obtained with high yield and satisfactory radiochemical purity. The biodistributions of ^99mTc/¹⁸⁸Re-labelled nanocapsules are close to those of classical PEG-coated particles and show good stability of ¹⁸⁸Re/^99mTc-SSS labelling.     

In vivo examination of 188Re(I)-tricarbonyl-labeled trastuzumab to target HER2-overexpressing breast cancer

IntroductionTrastuzumab (Herceptin), a humanized IgG1 monoclonal antibody directed against the extracellular domain of the HER2 protein, acts as an immunotherapeutic agent for HER2-overexpressing human breast cancers. Radiolabeled trastuzumab with β- or α emitters can be used as radioimmunotherapeutic agent for the similar purpose but with additional radiation effect.MethodsIn this study, trastuzumab was labeled with ¹⁸⁸Re for radioimmunotherapy of HER2/neu-positive breast cancer. ¹⁸⁸Re(I)-tricarbonyl ion, [¹⁸⁸Re(OH₂)₃(CO)₃]⁺, was employed as a precursor for directly labeling the monoclonal antibody with ¹⁸⁸Re. The immunoreactivity of ¹⁸⁸Re(I)-trastuzumab was estimated by competition receptor-binding assay using HER2/neu-overexpressive BT-474 human breast cancer cells. The localization properties of ¹⁸⁸Re(I)-trastuzumab within both tumor and normal tissues of athymic mice bearing BT-474 human breast cancer xenografts (HER2/neu-overexpressive) and similar mice bearing MCF-7 human breast cancer xenografts (HER2/neu-low expressive) were investigated.ResultsWhen incubated with human serum albumin and histidine at 25°C, ¹⁸⁸Re(I)-trastuzumab was found to be stable within 24 h. The IC₅₀ of ¹⁸⁸Re(I)-trastuzumab was found to be 22.63±4.57 nM. ¹⁸⁸Re(I)-trastuzumab was shown to accumulate specifically in BT-474 tumor tissue in in vivo biodistribution studies. By microSPECT/CT, the image of ¹⁸⁸Re localized BT-474 tumor was clearly visualized within 24 h. In contrast, ¹⁸⁸Re(I)-trastuzumab uptake in HER2-low-expressing MCF-7 tumor was minimal, and the ¹⁸⁸Re image at the localization of the tumor was dim.ConclusionThese results reveal that ¹⁸⁸Re(I)-trastuzumab could be an appropriate radioimmunotherapeutic agent for the treatment of HER2/neu-overexpressing cancers.     

Preparation and radiolabeling of human serum albumin (HSA)-coated magnetite nanoparticles for magnetically targeted therapy

In this paper, we describe the preparation of human serum albumin-coated magnetic particles of about 200 nm in diameter with narrow size distribution radiolabeled with ¹⁸⁸Re for the purpose of magnetically targeted therapy. The optimum radiolabeling conditions are: SnCl₂·2H₂O 8 mg/ml, citric acid 20 mg/ml, vitamin C 8 mg/ml, labeling volume 500 μl and a reaction time of 3 h. The stability of the radiolabeled particles is suitable for in vivo study.     

Effect of reaction conditions on preparations of rhenium-188 hydroxyethylidene diphosphonate complexes.

Rhenium-186 (Re-186) hydroxyethylidene diphosphonate (HEDP) has been shown to localize in metastatic foci within bone in a manner similar to Tc-99m bone-seeking agents. Usually, in the preparation of diagnostic Tc-99m radiopharmaceuticals, the concentration of Tc is at trace level (10(-8) M). However, large amounts of carrier are included in the preparation of Re-186 radiopharmaceuticals (10(-4) M), which may significantly affect the preparation of Re-HEDP. In this study, Re-188 was used as an Re tracer. The effects of pH and concentrations of Re carrier on the preparation of Re-HEDP were investigated. Re-188-Sn-HEDP was prepared by reconstitution of a kit of lyophilized HEDP mixture, and tin chloride with a radioactive solution of perrhenate in saline. The total concentration of Re present in this work ranged from 10(-8) to 10(-3) M. The results showed that high labeling efficiency was obtained for each preparation. Although the chemical behaviors of the Re-188 HEDP complexes, with and without carrier, were similar, the biodistribution patterns of carrier free Re-188 HEDP in rats were found to differ from the biodistribution patterns of carrier-added Re-188 HEDP.     

Synthesis and characterization of (99m)Tc- and (188)Re-complexes with a diamido-dihydroxymethylenephosphine-based bifunctional chelating agent (N(2)P(2)-BFCA).

A diamido-dihydroxymethylenephosphine (N(2)P(2)) bifunction chelating agent (BFCA) was shown to form well-defined (99m)Tc- and (188)Re-chelate structures. The 4, 4-bis [bis-hydroxymethyl-phosphonyl-propylcarbonmoyl]-butyric acid bifunctional chelating agent (N(2)P(2)-BFCA) formed stable complexes with (99m)Tc and (188)Re in >95% yield with high radiochemical purity (RCP). The biodistribution of the (99m)Tc- and (188)Re-N(2)P(2)-BFCAs after intravenous injection studied in normal mice showed the activity was excreted primarily via renal-urinary pathway indicating their use for labeling peptides with (99m)Tc and (188)Re.     

Rhenium-188 sulphur colloid as a radiation synovectomy agent

Radiation synovectomy has been shown to be an effective treatment for the rheumatoid arthritic knee. In this study, we evaluated the suitability of rhenium-188 as a radiation synovectomy agent. In addition, we were successful in labelling sulphur colloid with¹⁸⁸Re. In vitro stability tests revealed that more than 95% of the¹⁸⁸Re remained in colloid form over a 3-day period. Intra-articular injection of¹⁸⁸Re sulphur colloid into arthritic rabbit joints was followed by gamma camera imaging to quantify the leakage. The mean retention percentages of¹⁸⁸Re colloid in arthritic knees were 93.7% (±1.4%), 90.8% (±1.7%) and 87.2% (±0.6%) at 1 h, 1 day and 2 days, respectively. A biodistribution study of the arthritic rabbits revealed that the highest activity outside the knees was in the liver and the kidneys. Our preliminary results indicate that 188Re sulphur colloid may be an effective radiopharmaceutical for radiation synovectomy.     

188Re-胰岛素样生长因子1类似物在荷人胰腺癌裸鼠体内分布及其显像研究

目的 研究188Re标记胰岛素样生长因子l类似物(IGF-1A)在荷人胰腺癌裸鼠体内的分布及其显像.方法 ①直接法标记188Re-IGF-1A并测定标记率.②建立荷人胰腺癌Patu8988裸鼠模型.③188Re-IGF-1A经瘤内注射荷人胰腺癌裸鼠瘤内,分别于注射后15 min、1 h、4 h、24 h、3 d、5 d进行SPECT平面显像.④188ReO4-经瘤内注射后15 min、1 h、2 h、4 h、24 h进行显像,取各时间组裸鼠(n=4)脏器和肿瘤组织,计算每克组织百分注入剂量(%ID/g)及肿瘤/非肿瘤组织放射性摄取比值(T/NT).结果 ①188Re-IGF-1A标记率为(94.07±0.32)%.②瘤内注射188Re-IGF-1A后,肿瘤部位放射性积聚量4 h内差异无统计学意义(F=1.622,P＞0.05),且随时间延长,肿瘤与其他脏器的T/NT呈上升趋势,其中肿瘤/肌肉在5 d时最高,达到6531.79±4930.26.③瘤内注射188ReO4-后,在体内初始主要分布于甲状腺、胃、肿瘤、血液,随时间延长,肿瘤部位放射性计数迅速下降.④在24 h,瘤内注射188Re-IGF-1A组肿瘤及肾脏内%ID/g较188ReO4-组高,两者有统计学差异(t=5.877,t=13.287,P＜0.01);两组肿瘤内%ID/g比值在24 h达到最高,为74.10倍.⑤瘤内注射188Re-IGF-1A后,SPECT平面显像见瘤内浓聚,5 d时仅见肿瘤部位显影.结论 188Re-IGF-1A对胰腺癌具有良好的亲和力,在肿瘤部位有较高的T/NT,可望作为胰腺癌治疗的药物.