文獻(xiàn)：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

文獻(xiàn)鏈接：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. 

開發(fā)了一種新型的PEG免疫脂質(zhì)體，在PEG鏈的遠(yuǎn)端攜帶單克隆抗體或其片段（F（ab′）2，F(xiàn)ab′）（C型）。聚乙二醇二硬脂酰磷脂酰乙醇胺衍生物?新合成了PEG末端帶有馬來酰亞胺基的烷基（DSPE-PEG-COOH）或二棕櫚酰磷脂酰乙醇胺衍生物（DPPE-PEG-Mal）。

由含有6mol%DSPE-PEG-COOH或DPPE-PEG-Mal的二硬脂酰磷脂酰膽堿和膽固醇（2:1，m/m）制備了小單層脂質(zhì)體（直徑90-130nm）。為了靶向血管內(nèi)皮肺表面作為模型可及位點(diǎn)，將對(duì)小鼠肺內(nèi)皮細(xì)胞高度特異性的34A抗體與PEG脂質(zhì)體（34A C型）結(jié)合。

BALB/C小鼠中34A C型的肺結(jié)合程度明顯高于普通型免疫脂質(zhì)體（不含PEG衍生物）34A A型。為了靶向?qū)嶓w瘤組織作為不易接近部位的模型，使用了抗人CEA的21B2抗體及其Fab′片段。

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