Gupta H, Wilkinson R A, Bogdanov A A, Callahan R J, Weissleder R
Department of Radiology, Massachusetts General Hospital, Charlestown 02129, USA.
Radiology. 1995 Dec;197(3):665-9. doi: 10.1148/radiology.197.3.7480736.
To test whether a nontargeted, long-circulating, synthetic polymer accumulates in areas of inflammation, with high capillary permeability and increased regional blood flow.
Methoxy poly(ethylene glycol)-poly-L-lysine (PL)-diethylenetriaminepentaacetic acid (MPEG-PL-DTPA) was labeled with technetium-99m for scintigraphy and with gadolinium for magnetic resonance (MR) imaging. Eleven Escherichia coli-infected rats were injected with 1.0 mCi (37 MBq) of Tc-99m-labeled MPEG-PL-DTPA for scintigraphy. Twelve rats underwent 1.5-T MR imaging after intravenous injection of gadolinium-labeled MPEG-PL-DTPA (35 mumol/kg).
Tc-99m-labeled MPEG-PL-DTPA demonstrated nearly eight-fold higher accumulation in infected muscle when compared with normal muscle. Scintigrams and MR images showed areas of inflammation with peak accumulation at 24 hours after injection of Tc-99m- or gadolinium-labeled MPEG-PL-DTPA.
Nontargeted, long-circulating, copolymers can efficiently accumulate in sites of inflammation and thus represent an alternative to inflammation-specific agents.
测试一种非靶向、长循环的合成聚合物是否会在炎症区域蓄积，这些区域具有高毛细血管通透性和增加的局部血流。
甲氧基聚（乙二醇）-聚-L-赖氨酸（PL）-二乙三胺五乙酸（MPEG-PL-DTPA）用99m锝标记用于闪烁显像，用钆标记用于磁共振（MR）成像。11只感染大肠杆菌的大鼠注射1.0毫居里（37兆贝可）的99mTc标记的MPEG-PL-DTPA用于闪烁显像。12只大鼠在静脉注射钆标记的MPEG-PL-DTPA（35微摩尔/千克）后进行1.5-T MR成像。
与正常肌肉相比，99mTc标记的MPEG-PL-DTPA在感染肌肉中的蓄积量高出近8倍。闪烁显像图和MR图像显示炎症区域在注射99mTc或钆标记的MPEG-PL-DTPA后24小时达到蓄积峰值。
非靶向、长循环的共聚物可有效蓄积于炎症部位，因此可作为炎症特异性药物的替代品。
