文献：Targeted delivery and triggered release of liposomal doxorubicin enhances cytotoxicity against human B lymphoma cells

作者：T Ishida a 1, M.J Kirchmeier a 2, E.H Moase a, S Zalipsky b, T.M Allen 

文献链接：

https://www.sciencedirect.com/science/article/pii/S0005273601004096

摘要：

DOPE liposomes can also be stabilized in the bilayer state by an amphiphile with bulky and/or charge-repulsing hydrophilic moieties [35]. CHEMS (cholesteryl hemisuccinate), which is net negatively charged at pH 7.4, has been widely used to stabilize DOPE in the bilayer state at neutral pH. Protonation of CHEMS at low pH (<6.0) accelerates the destabilization of DOPE vesicles by promoting the formation of the hexagonal (HII) phase [16], [36]. DOPE/CHEMS formulations without mPEG-DSPE had little leakage at pH 7.4, but rapidly released encapsulated dye at pH 5.5 (Fig. 2A). At pH 5.5 or 7.4 less than 10% leakage occurred over 24 h when these liposomes were stabilized with 5 mol% mPEG-DSPE (Fig. 2A). In the presence of DTT, DOPE/CHEMS liposomes containing 5 mol% mPEG-S-S-DSPE had a release half-life of approximately 8 h at pH 5.5, while little release occurred at pH 7.4 (Fig. 2B); DTT treatment of DOPE/CHEMS liposomes stabilized with 3 mol% mPEG-S-S-DSPE resulted in intermediate leakage rates

DOPE脂质体也可以通过具有大体积和/或电荷排斥亲水部分的两亲性物在双层状态下稳定。CHEMS（胆固醇半琥珀酸盐）在pH 7.4时带净负电荷，已被广泛用于在中性pH下稳定双层状态的DOPE。

CHEMS在低pH（<6.0）下的质子化通过促进六方（HII）相的形成加速了DOPE囊泡的失稳。不含mPEG-DSPE的DOPE/CHEMS制剂在pH 7.4时几乎没有泄漏，但在pH 5.5时迅速释放包封染料。

在pH 5.5或7.4下，当这些脂质体用5mol%mPEG-DSPE稳定时，24小时内发生的泄漏小于10%。在DTT存在的情况下，含有5mol%mPEG-S-S-DSPE的DOPE/CHEMS脂质体在pH 5.5时的释放半衰期约为8小时，而在pH 7.4时几乎没有释放（图2B）；用3mol%mPEG-S-S-DSPE稳定的DOPE/CHEMS脂质体的DTT处理导致中等泄漏率。

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