文献：带有聚乙二醇偶联 Fab′ 片段的免疫脂质体在体内循环时间延长，并能高度渗入目标实体*

链接：https://febs.onlinelibrary.wiley.com/doi/full/10.1016/S0014-5793%2897%2900905-8

作者：丸山和夫， 高桥伸也， 田川俊明， 永池一宏， 岩鹤元治

节选：

我们开发了一种新型长循环免疫脂质体（Fab′-PEG免疫脂质体），可高效地渗入体内靶向实体*。我们以二硬脂酰磷脂酰胆碱（DSPC）、胆固醇（CHOL）、末端带有马来酰亚胺基的PEG二棕榈酰磷脂酰乙醇胺衍生物（DPPE-PEG-Mal）以及偶联的*体Fab′片段，制备了直径100-130纳米的小型单层脂质体。DPPE-PEG-Mal的引入以及Fab′片段（而非完整*体）与PEG末端的连接，使得脂质体能够避开RES的摄取，并在循环中停留更长时间，从而增强脂质体在实体*中的蓄积。由于这种 Fab′-PEG 免疫脂质体能够靶向实体*，因此它们不仅可以作为化疗药物的载体，而且可以作为大分子药物的载体，具有很高的吸引力。

Abstract

We have 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.

西安齐岳生物提供相关产品：

DSPE-PEG-T7(HAIYPRH)

DPPE-ICG

DSPE-PEG-FITC

DSPE-PEG-CTT2

DSPE-PEG-Methyltetrazine

DPPE-Cap-Folate

DSPE-PEG-PTP

DSPE-Rhodamine B/DSPE-RhB

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