文献：Immunoliposomes bearing polyethyleneglycol-coupled Fab' fragment show prolonged circulation time and high extravasation into targeted solid tumors in vivo.

文献链接：https://xueshu.baidu.com/usercenter/paper/show?paperid=f7bc93636f643c6b3070f00ae89708d5&site=xueshu_se

作者：K Maruyama，N Takahashi，T Tagawa，K Nagaike，M Iwatsuru

摘要：

developed a new type of long-circulating immunoliposome (Fab'-PEG immunoliposomes) which is efficiently extravasated into the targeted solid tumor in vivo. Small unilamellar liposomes (100-130 nm in diameter) were prepared from distearoylphosphatidylcholine (DSPC), cholesterol (CHOL) and a dipalmitoylphosphatidylethanolamine derivative of PEG with a terminal maleimidyl group (DPPE-PEG-Mal), and conjugated Fab' fragment of antibody. Inclusion of DPPE-PEG-Mal and linkage of the Fab' fragment instead of intact antibody to PEG terminals allowed the liposomes to evade RES uptake and remain in the circulation for a long time, resulting in enhanced accumulation of the liposomes in the solid tumor. Because of the ability of such Fab'-PEG immunoliposomes to target solid tumors, they appear highly attractive as carriers of not only chemotherapeutic agents, but also of macromolecular drugs.

开发了一种新型的长循环免疫脂质体（Fab'-PEG免疫脂质体），可在体内有效地外渗到靶向实体瘤中。由二硬脂酰磷脂酰胆碱（DSPC）、胆固醇（CHOL）和具有末端马来酰亚胺基的PEG的二棕榈酰磷脂酰乙醇胺衍生物（DPPE-PEG-Mal）制备小单层脂质体（直径100-30nm），并偶联抗体的Fab’片段。

包含DPPE-PEG-Mal并将Fab’片段而不是完整抗体连接到PEG末端，使脂质体能够逃避RES摄取并长时间留在循环中，从而增强脂质体在实体瘤中的积聚。

由于这种Fab'-PEG免疫脂质体靶向实体瘤的能力，它们不仅作为化疗药物的载体，而且作为大分子药物的载体都具吸引力。

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