Current Drug Delivery

Author(s): Yao-Hua Ouyang, Wei Xu, Cheng-Kai Zhou, Fan Liu, Bin Li, Guo-Ping Yan*, Lian Yang, Si Chen and Can Jiang

DOI: 10.2174/1567201815666180409111005

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Porphyrin-containing Gadolinium Complex as a Tumor-targeting Magnetic Resonance Imaging (MRI) Contrast Agent

Page: [972 - 978] Pages: 7

  • * (Excluding Mailing and Handling)

Abstract

Objective: Gadolinium diethylenetriaminepentaacetic di[5-(4’-amidophenyl)-10,15,20- tris(4’-sulfonatophenyl) porphyrin trisodium salt] (Gd-DTPA-2APTSPP) was synthesized by the reaction of diethylenetriaminepentaacetic dianhydride with 5-(4’-aminophenyl)-10,15,20-tris(4’-sulfonatophenyl) porphyrin and subsequently chelation with gadolium chloride.

Methods: This gadolinium complex was characterized and its properties in vitro and in vivo were also evaluated. Compared with Gd-DTPA, Gd-DTPA-2APTSPP possessed high relaxivity r1, low cytotoxicity to HeLa cells and high enhanced signal intensities of the VX2 carcinoma in rabbits for a prolonged time.

Conclusion: Moreover, Gd-DTPA-2APTSPP can distinguish the VX2 carcinoma from the reactive hyperplasia incited by inflammation and normal tissues in rabbits. Therefore, Gd-DTPA-2APTSPP can be taken up selectively by tumors and show the potential as a tumor-targeting MRI contrast agent.

Keywords: Magnetic resonance imaging (MRI), contrast agent, gadolinium complex, porphyrin, VX2 carcinoma, tumortargeting.

Graphical Abstract