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不同mPEG-DSPE衍生物对脂质体释放动力学的影响
发布时间:2025-07-11     作者:zyl   分享到:
资料:Targeted delivery and triggered release of liposomal doxorubicin enhances cytotoxicity against human B lymphoma cells小编:T Ishida a 1, M.J Kirchmeier a 2, E.H Moase a, S Zalipsky b, T.M Allen 医学文献外部链接:

结语: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

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DOPE脂质体也能够 实现具备有总的积和/或正电势讨厌亲水的部分的两亲性物在单层程序下稳固可靠。CHEMS(固醇半虎珀酸盐)在pH 7.4时带净负正电势,已被常见用在在比较适中pH下稳固可靠单层程序的DOPE。CHEMS在低pH(<6.0)下的质子化可以通过推进六方(HII)相的造成减速了DOPE囊泡的失稳。不标mPEG-DSPE的DOPE/CHEMS药物在pH 7.4时基本上不会有用户名,但在pH 5.5时及时释放出来包封染色剂。

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。

对应安利:N3-PEG-SGPhosphoric acid-PEG-N3N3-PEG-PAA(1.8K)-DAN3-PEG-NHSN3-PEG-AlkeneACA-PEG-N3AC-PEG-N3AlKyne-PEG-N3COOH-PEG-N3MA-PEG-N3N3-PEG-EPON3-PEG-OHN3-PEG-SHCHO-PEG-N3N3-PEG-NH2之上散文內容特征各样杂志或资料,如果侵犯知识产权请结合企业删除文件!