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

文獻(xiàn)鏈接：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.

開(kāi)發(fā)了一種新型的長(zhǎng)循環(huán)免疫脂質(zhì)體（Fab'-PEG免疫脂質(zhì)體），可在體內(nèi)有效地外滲到靶向?qū)嶓w瘤中。由二硬脂酰磷脂酰膽堿（DSPC）、膽固醇（CHOL）和具有末端馬來(lái)酰亞胺基的PEG的二棕櫚酰磷脂酰乙醇胺衍生物（DPPE-PEG-Mal）制備小單層脂質(zhì)體（直徑100-30nm），并偶聯(lián)抗體的Fab’片段。

包含DPPE-PEG-Mal并將Fab’片段而不是完整抗體連接到PEG末端，使脂質(zhì)體能夠逃避RES攝取并長(zhǎng)時(shí)間留在循環(huán)中，從而增強(qiáng)脂質(zhì)體在實(shí)體瘤中的積聚。

由于這種Fab'-PEG免疫脂質(zhì)體靶向?qū)嶓w瘤的能力，它們不僅作為化療藥物的載體，而且作為大分子藥物的載體都具吸引力。

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DSPE-PEG-c(RGDyK)

DSPE-PEG-CHEMS

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