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用铟-111标记的空间稳定脂质体用于成像局灶性感染。

Sterically stabilized liposomes labeled with indium-111 to image focal infection.

作者信息

Boerman O C, Storm G, Oyen W J, van Bloois L, van der Meer J W, Claessens R A, Crommelin D J, Corstens F H

机构信息

Department of Nuclear Medicine, University Hospital, Nijmegen, The Netherlands.

出版信息

J Nucl Med. 1995 Sep;36(9):1639-44.

PMID:7658225
Abstract

UNLABELLED

To determine the potential of sterically stabilized liposomes to image infectious and inflammatory foci, the in vivo behavior of 111In-labeled PEGylated (coated with polyethylene glycol) liposomes was studied in a rat model.

METHODS

Indium-111-PEGylated lipsomes were administered intravenously to rats infected with S. aureus in the left calf muscle. The distribution of the radiolabel was studied by gamma counting of dissected tissues and gamma camera imaging for 48 hr. As a reference agent, the preparation of 111In-IgG was included in these studies.

RESULTS

Clearance of the PEGylated liposomes from the blood compartment was similar to the clearance of 111In-IgG in this model (t1/2 approximately 20 hr). Uptake of the radiolabel in the abscess with the 111In-liposomes was twice as high as the uptake following injection of 111In-IgG (2.7%ID/g versus 1.1%ID/g at 48 hr postinjection). Tissue counting revealed that abscess-to-muscle ratios reached values up to 20 and 34 (24 and 48 p.i., respectively). As early as 1 hr postinjection, the abscess could be visualized scintigraphically.

CONCLUSION

The in vivo characteristics of this liposomal formulation in this rat model indicate that sterically stabilized liposomes labeled with gamma emitters might be a valuable addition to the arsenal of radiopharmaceuticals currently used for infection imaging.

摘要

未标记

为了确定空间稳定脂质体对感染性和炎症病灶成像的潜力,在大鼠模型中研究了111In标记的聚乙二醇化(涂有聚乙二醇)脂质体的体内行为。

方法

将铟-111-聚乙二醇化脂质体静脉注射到左小腿肌肉感染金黄色葡萄球菌的大鼠体内。通过对解剖组织进行γ计数和γ相机成像研究放射性标记物的分布,持续48小时。作为参考剂,这些研究中包括111In-IgG制剂。

结果

在该模型中,聚乙二醇化脂质体从血液中的清除与111In-IgG的清除相似(半衰期约为20小时)。111In-脂质体在脓肿中的放射性标记物摄取量是注射111In-IgG后摄取量的两倍(注射后48小时分别为2.7%ID/g和1.1%ID/g)。组织计数显示脓肿与肌肉的比率分别达到20和34(分别在注射后24和48小时)。早在注射后1小时,脓肿就可以通过闪烁显像观察到。

结论

该脂质体制剂在该大鼠模型中的体内特性表明,用γ发射体标记的空间稳定脂质体可能是目前用于感染成像的放射性药物库中的一个有价值的补充。

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