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  • the degradation and clearance of poly(n-hydroxypropyl-l-glutamine)-dtpa-gd as a blood pool mri contrast agent

    جزئیات بیشتر مقاله
    • تاریخ ارائه: 1391/01/01
    • تاریخ انتشار در تی پی بین: 1391/01/01
    • تعداد بازدید: 894
    • تعداد پرسش و پاسخ ها: 0
    • شماره تماس دبیرخانه رویداد: -

    although polymeric magnetic resonance imaging (mri) agents have significantly improved relaxivity and prolonged circulation time in vivo compared with current imaging agents, the potential for long-term toxicity prevents their translation into the clinic. the aim of this study was to develop a new biodegradable, nonionic polymeric blood pool mri contrast agent with efficient clearance from the body. we synthesized phpg-dtpa, which possesses two potentially degradable sites in vivo: protein amide bonds of the polymer backbone susceptible to enzymatic degradation and hydrolytically labile ester bonds in the side chains. after chelation with gd3+, phpg-dtpa-gd displayed an r1 relaxivity of 15.72 mm−1⋅sec−1 (3.7 times higher than that of magnevistt). in vitro, dtpa was completely released from phpg polymer within 48 h when incubated in mouse plasma. in vivo, phpg-dtpa-gd was cleared via renal route as shown by micro-single photon emission computed tomography of mice after intravenous injection of 111in-labeled phpg-dtpa-gd. mri of nude rats bearing c6 glioblastoma showed significant enhancement of the tumor periphery after intravenous injection of phpg-dtpa-gd. furthermore, mouse brain angiography was clearly delineated up to 2 h after injection of phpg-dtpa-gd. phpg-dtpa-gd’s biodegradability, efficient clearance, and significantly increased relaxivity make it a promising polymeric blood pool mri contrast agent.

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