PEG-g-poly(GdDTPA-co-L-cystine): A Biodegradable Macromolecular Blood Pool Contrast Agent for MR Imaging

详细信息    查看全文

• 作者：Aaron M. Mohs ; Xinghe Wang ; K. Craig Goodrich ; Yuda Zong ; Dennis L. Parker ; and Zheng-Rong Lu
• 刊名：Bioconjugate Chemistry
• 出版年：2004
• 出版时间：November 2004
• 年：2004
• 卷：15
• 期：6
• 页码：1424 - 1430
• 全文大小：291K
• 年卷期：v.15,no.6(November 2004)
• ISSN：1520-4812

文摘

Biodegradable PEGylated Gd-DTPA L-cystine copolymers, PEG-g-poly(GdDTPA-co-L-cystine), wereprepared and tested as a blood pool contrast agent in mice. The biodegradable macromolecular agentwas designed to be broken down into smaller Gd complexes by endogenous thiols via the disulfide-thiol exchange reaction to facilitate the clearance of Gd complexes after the contrast-enhanced MRIexamination. Gd-DTPA L-cystine copolymers were synthesized by condensation polymerization ofL-cystine and DTPA-dianhydride in water followed by chelating with Gd(OAc)₃. MPEG-NH₂ (MW =2000) was then conjugated to the polymeric backbone in different ratios. The macromolecular contrastagent was readily degraded with the incubation of L-cysteine. It also demonstrated superior contrastenhancement in the heart and blood vessels as compared to a low molecular weight control agent,Gd-(DTPA-BMA). At 1 h postcontrast, the PEGylated macromolecular agent still showed prominentenhancement, while little contrast enhancement was detectable in the blood pool by the control agent.PEG-g-poly(GdDTPA-co-L-cystine) shows promise as an MR blood pool imaging agent.