文献：Targeting efficiency of PEG-immunoliposome-conjugated antibodies at PEG terminals

作者：

Kazuo Maruyama a, Tomoko Takizawa a, Nobuya Takahashi a, Toshiaki Tagawa b, Kazuhiro Nagaike b, Motoharu Iwatsuru

文献链接：https://www.sciencedirect.com/science/article/abs/pii/S0169409X96004632

摘要：

We have developed a new type of PEG-immunoliposome carrying monoclonal antibodies or their fragments (F(ab′)2, Fab′) at the distal ends of the PEG chains (Type C). Distearoylphosphatidylethanolamine derivatives of PEG with car☐yl group (DSPE-PEG-COOH) or dipalmitoyl phosphatidylethanolamine derivatives of PEG with maleimidyl group (DPPE-PEG-Mal) at the PEG terminal were newly synthesized. Small unilamellar liposomes (90–130 nm in diameter) were prepared from distearoyl phosphatidylcholine and cholesterol (2:1, m/m) containing 6 mol% of DSPE-PEG-COOH or DPPE-PEG-Mal. To target to the vascular endothelial lung surface as a model accessible site, 34A antibody, which is highly specific to mouse pulmonary endothelial cells, was conjugated to PEG-liposome (34A-Type C). The degree of lung binding of 34A-Type C in BALB/c mice was significantly higher than that of the 34A-Type A which is an ordinary type immunoliposome (without PEG derivatives). To target to the solid tumor tissue as a model of the less accessible site, 21B2 antibody which is anti-human CEA and its Fab′ fragment were used. 

开发了一种新型的PEG免疫脂质体，在PEG链的远端携带单克隆抗体或其片段（F（ab′）2，Fab′）（C型）。聚乙二醇二硬脂酰磷脂酰乙醇胺衍生物☐新合成了PEG末端带有马来酰亚胺基的烷基（DSPE-PEG-COOH）或二棕榈酰磷脂酰乙醇胺衍生物（DPPE-PEG-Mal）。

由含有6mol%DSPE-PEG-COOH或DPPE-PEG-Mal的二硬脂酰磷脂酰胆碱和胆固醇（2:1，m/m）制备了小单层脂质体（直径90-130nm）。为了靶向血管内皮肺表面作为模型可及位点，将对小鼠肺内皮细胞高度特异性的34A抗体与PEG脂质体（34A C型）结合。

BALB/C小鼠中34A C型的肺结合程度明显高于普通型免疫脂质体（不含PEG衍生物）34A A型。为了靶向实体瘤组织作为不易接近部位的模型，使用了抗人CEA的21B2抗体及其Fab′片段。

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mPEG-di-Glutamic Acid

mPEG-FA

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mPEG-SBA

mPEG-PCL(3K)

mPEG-SS-C30

mPEG-PCL(10K)

mPEG-PCL(12K)

mPEG-Alkene

mPEG-DF

mPEG-DBCO

mPEG-DA

mPEG-Dansyl

mPEG-Ts 

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