标题:山萘酚靶向脂质体的制备与评价
链接:https://xueshu.baidu.com/usercenter/paper/show?paperid=7798a3dbd8f6faa67daba37ba632887f&site=xueshu_se
作者:刘祖浩,雷玉杰,宋浩颖,常聪
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).
译文:
我们开发了一种新型的PEG免疫脂质体,在PEG链的远端携带单克隆*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*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。
DOI:10.3969/j.issn.1008-987x.2021.03.09
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