文獻：PEG-Immunoliposome 

作者：Kazuo Maruyama

文獻鏈接：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.

本文綜述了新開發的懸垂型PEG免疫脂質體（C型）的現狀，該脂質體在PEG鏈的遠端攜帶單克隆抗體或其片段（Fab’）。就C型的靶結合而言，考慮了兩個不同的解剖區室。

它們是小鼠肺內皮，作為通過血管內途徑容易到達的部位，以及植入的實體瘤，作為通過外滲到達的不太容易到達的目標部位。由含有6mol%DSPE-PEG-COOH或DPPE-PEG-Mal的磷脂酰膽堿和膽固醇（2:1，m/m）制備小單層脂質體（直徑90-130nm）。為了靶向肺血管內皮表面，將對小鼠肺內皮細胞高度特異的34A抗體與PEG脂質體（34A C型）結合。

在BALB/C小鼠中，34A C型的肺結合程度顯著高于34A A型，后者是一種普通的免疫脂質體（不含PEG衍生物）。為了靶向實體瘤組織，使用了21B2抗體（抗人CEA）及其Fab’片段。Fab'-C型顯示低RES攝取和長循環時間，并且可以看到脂質體在實體瘤中的積累增強。

小Fab’-C型主要通過被動對流運輸穿過泄漏的腫瘤內皮。這些研究為C型脂質體靶向藥物遞送的潛力提供了重要見解。

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