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188Re-bMEDA-脂质体在C26小鼠结肠癌实体瘤动物模型中的生物分布、药代动力学及显微单光子发射计算机断层扫描/计算机断层扫描成像

Biodistribution, pharmacokinetics and microSPECT/CT imaging of 188Re-bMEDA-liposome in a C26 murine colon carcinoma solid tumor animal model.

作者信息

Chang Ya-Jen, Chang Chih-Hsien, Chang Tsui-Jung, Yu Chia-Yu, Chen Liang-Cheng, Jan Meei-Lin, Luo Tsai-Yueh, Lee Te-Wei, Ting Gann

机构信息

Institute of Nuclear Energy Research, Taoyuan, Taiwan, ROC.

出版信息

Anticancer Res. 2007 Jul-Aug;27(4B):2217-25.

Abstract

Nanoliposomes are useful carriers in drug delivery. Radiolabeled nanoliposomes have potential applications in radiotherapy and diagnostic imaging. In this study, the biodistribution and pharmacokinetics of 188Re-BMEDA-labelled pegylated liposomes (RBLPL) and unencapsulated 188Re-BMEDA administered by the i.v. route in murine C26-colon tumour-bearing mice were investigated. MicroSPECT/CT images were performed to evaluate the distribution and tumor targeting of RBLPL in mice. For the biodistribution study, the highest uptake of liposome in tumors was 3.62% +/- 0.73% at 24 h after RBLPL administration, and the tumor to muscle ratio of RBLPL was 7.1-fold higher than that of 188Re-BMEDA. With image analysis, the highest SUV in tumor was 2.81 +/- 0.26 at 24 h after injection of RBLPL. The Pearson correlation analysis showed a positive correlation of tumor targeting or uptake of RBLPL between biodistribution and microSPECT semi-quantification imaging analysis (r = 0.633). The results of the pharmacokinetics revealed that the area under the tissue concentration-time curve (AUC) of RBLPL was 4.7-fold higher than that of unencapsulated 188Re-BMEDA. These results suggested the potential benefit and advantage of 188Re-labeled nanoliposomes for imaging and treatment of malignant diseases.

摘要

纳米脂质体是药物递送中有用的载体。放射性标记的纳米脂质体在放射治疗和诊断成像中具有潜在应用。在本研究中,研究了静脉注射188Re-BMEDA标记的聚乙二醇化脂质体(RBLPL)和未包封的188Re-BMEDA在荷C26结肠癌小鼠中的生物分布和药代动力学。进行了MicroSPECT/CT成像以评估RBLPL在小鼠体内的分布和肿瘤靶向性。在生物分布研究中,RBLPL给药后24小时肿瘤中脂质体的最高摄取量为3.62%±0.73%,RBLPL的肿瘤与肌肉比值比188Re-BMEDA高7.1倍。通过图像分析,注射RBLPL后24小时肿瘤中的最高SUV为2.81±0.26。Pearson相关性分析显示生物分布与MicroSPECT半定量成像分析之间RBLPL的肿瘤靶向或摄取呈正相关(r = 0.633)。药代动力学结果显示,RBLPL的组织浓度-时间曲线下面积(AUC)比未包封的188Re-BMEDA高4.7倍。这些结果表明188Re标记的纳米脂质体在恶性疾病成像和治疗方面具有潜在益处和优势。

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