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药学学报  2015 

spio-shrna双功能分子探针药动学及活体mr成像研究

, PP. 1285-1289

Keywords: 药代动力学,分子探针,超顺磁性氧化铁,磁共振成像

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Abstract:

本研究探讨spio-shrna双功能分子探针在活体内的药代动力学特征及磁共振(magneticresonance,mr)成像无创评估其主要脏器分布。将18只新西兰大白兔随机分为3组,分别注射不同剂量的分子探针,于注射前30min及注射后不同时间点采血,测量铁含量以分析探针药代动力学。24只昆明(km)小鼠随机分为4组,以每只小鼠尾静脉注射200μl生理盐水为对照组,另3组分别注射不同剂量的分子探针,于注射后24h行mri扫描,扫描结束后立即取肝、脾、肾、脑及肌肉,制作切片行普鲁士蓝染色,观察探针在体内主要脏器组织的分布情况。结果显示,本探针的药代动力学符合二室模型,半衰期超过3h;mri显示探针在正常小鼠体内主要分布于肝脏与脾脏,肝脾mri信号随着探针剂量的增加而降低(均p<0.05),组织切片普鲁士蓝染色证实了mri检查结果,同时显示探针绝大部分能够逃避单核吞噬细胞系统的吞噬。本研究明确了spio-shrna分子探针在动物体内的药代动力学及主要脏器分布,为进一步的肿瘤活体成像时间及剂量的选择提供了重要参考价值。

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