文献：PEG-Immunoliposome 

作者：Kazuo Maruyama

文献链接：https://portlandpress.com/bioscirep/article-abstract/22/2/251/55027/PEG-Immunoliposome

摘要：

This review deals with the current status of newly developed pendant-type PEG-immunoliposomes (Type C), carrying monoclonal antibodies or their fragments (Fab') at the distal ends of the PEG chains. In terms of target binding of Type C, two different anatomical compartments are considered. They are mouse lung endothelium as a readily accessible site via the intravascular route and the implanted solid tumor as a much less accessible target site reached via extravasation. Small unilamellar liposomes (90–130 nm in diameter) were prepared from phosphatidycholine and cholesterol (2:1, m/m) containing 6 mol.% of DSPE-PEG-COOH or DPPE-PEG-Mal. For targeting to the vascular endothelial surface in the lung, 34A antibody, which is highly specific to mouse pulmonary endothelial cells, was conjugated to PEG-liposomes (34A-Type C). The degree of lung binding of 34A-Type C in BALB/c mouse was significantly higher than that of 34A-Type A, which is an ordinary type of immunoliposome (without PEG derivatives). For targeting to solid tumor tissue, 21B2 antibody (anti-human CEA) and its Fab' fragment were used. The targeting ability of Fab'-Type C was examined by using CEA-positive human gastric cancer strain MKN-45 cells inoculated into BALB/c nu/nu mice. Fab'-Type C showed low RES uptake and a long circulation time, and enhanced accumulation of the liposomes in the solid tumor was seen. The small Fab'-Type C predominantly passed through the leaky tumor endothelium by passive convective transport. These studies offer important insights into the potential of Type C liposomes for target-specific drug delivery.

本文综述了新开发的悬垂型PEG免疫脂质体（C型）的现状，该脂质体在PEG链的远端携带单克隆抗体或其片段（Fab’）。就C型的靶结合而言，考虑了两个不同的解剖区室。

它们是小鼠肺内皮，作为通过血管内途径容易到达的部位，以及植入的实体瘤，作为通过外渗到达的不太容易到达的目标部位。由含有6mol%DSPE-PEG-COOH或DPPE-PEG-Mal的磷脂酰胆碱和胆固醇（2:1，m/m）制备小单层脂质体（直径90-130nm）。为了靶向肺血管内皮表面，将对小鼠肺内皮细胞高度特异的34A抗体与PEG脂质体（34A C型）结合。

在BALB/C小鼠中，34A C型的肺结合程度显著高于34A A型，后者是一种普通的免疫脂质体（不含PEG衍生物）。为了靶向实体瘤组织，使用了21B2抗体（抗人CEA）及其Fab’片段。Fab'-C型显示低RES摄取和长循环时间，并且可以看到脂质体在实体瘤中的积累增强。

小Fab’-C型主要通过被动对流运输穿过泄漏的肿瘤内皮。这些研究为C型脂质体靶向药物递送的潜力提供了重要见解。

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