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DSPE-PEG-COOH封端脂质体表面偶联PPACK肽的策略及其稳定性研究
发布时间:2025-07-09     作者:zyl   分享到:

文献:BioMed Research International

文献链接:https://onlinelibrary.wiley.com/doi/full/10.1155/2014/129458

摘要:

Postmodification of the liposome surface by amine-carboxyl conjugation (Figure 1(b)) was recently reported to overcome the rapid systemic clearance of D-phenylalanyl-L-prolyl-L-arginyl-chloromethyl ketone short peptide (PPACK), an antithrombin agent [30]. Palekar et al.  demonstrated that PPACK peptide is attached to the surface of preformed liposomes composed of EPC, DPPE, and DSPE-PEG2000-COOH (94 : 4 : 2 molar ratio) by applying standard amine-carboxyl coupling conditions for conjugating the N-terminus of the peptide to preformed carboxy-terminated DSPE-PEG-containing liposomes. The peptide was conjugated to the unilamellar liposomes and liposomes were purified by dialysis for four hours, which suggests high stability of the nanosystem. 

通过胺羧基偶联对脂质体表面进行后修饰,可以克服抗凝血酶剂D-苯丙氨酰-L-脯氨酰基-L-精氨酰氯甲基酮短肽(PPACK)的快速全身清除。Palekar等人通过应用标准胺羧基偶联条件将肽的N端偶联到预先形成的含羧基封端的DSPE-PEG的脂质体上,证明了PPACK肽附着在由EPC、DPPE和DSPE-PEG2000-COOH(94:4:2摩尔比)组成的预先形成的脂质体的表面上。肽与单层脂质体结合,脂质体通过透析4小时纯化,这表明纳米系统具有很高的稳定性。

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