A high relaxivity Gd(III)DOTA-DSPE-based liposomal contrast agent for magnetic resonance imaging
A high relaxivity Gd(III)DOTA-DSPE-based liposomal contrast agent for magnetic resonance imaging
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DOI：
10.1016/j.ejpb.2008.09.017
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发表时间：
2009-06-01
影响因子：
4.9
通讯作者：
Nicolay, Klaas
中科院分区：
文献类型：
--
作者：
Hak, Sjoerd;Sanders, Honorius M. H. F.;Nicolay, Klaas
分子成像领域的目标是在细胞和分子水平上可视化和量化（病理）生理过程。采用敏感的和位点靶向的造影剂来可视化感兴趣的过程的分子成分。本研究的主要目的是开发一种磁共振成像（MRI）检测脂质体具有高弛豫性和稳定性。为此，合成Gd（III）DOTA-DSPE并掺入脂质体制剂中。所得脂质体在造影剂效率和结构特性方面进行了广泛的体外表征。脂质体显示出具有高的纵向弛豫率，这对于在分子成像研究中检测低浓度分子标记物是至关重要的。我们还证明了Gd（III）DOTA-DSPE在与Zn（II）孵育后没有表现出可检测的transmethalo。这一点很重要，因为它显著有助于造影剂的生物相容性。本脂质体制剂将作为分子成像和靶向药物递送研究的通用和良好表征的平台。(C)2008 Elsevier B. V.保留所有权利。
The field of molecular imaging aims to visualize and quantify (patho)physiological processes at the cellular and molecular level. Sensitive and site-targeted contrast agents are employed to visualize molecular constituents of processes of interest. The principal aim of this study was to develop a magnetic resonance imaging (MRI) detectable liposome with high relaxivity and stability. To this end, Gd(III)DOTA-DSPE was synthesized and incorporated in a liposomal formulation. The resulting liposomes were extensively characterized in vitro in terms of contrast agent efficiency and structural properties. The liposomes were shown to have a high longitudinal relaxivity, which is crucial for the detection of low concentration molecular markers in molecular imaging studies. We also demonstrated that Gd(III)DOTA-DSPE exhibits no detectable transmetallation upon incubation with Zn(II). This is important as it significantly contributes to the biocompatibility of the contrast agent. The present liposome preparation will serve as versatile and well characterized platform for molecular imaging and targeted drug delivery studies. (C) 2008 Elsevier B.V. All rights reserved.