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：

Since CFE is expected to contain cytoplasmic and lysosomal enzymes, the leakage of the hydrophilic, membrane-impermeable dye HPTS from formulations exposed to CFE may mimic the process of destabilization, in an intracellular environment, of liposomes stabilized with either mPEG-DSPE or mPEG-S-S-DSPE. CFE was adjusted to pH 5.5, approximating the lysosomal pH of between 5 and 6.5 [37], [38]. DOPE formulations, or DOPE formulations with 3 mol% mPEG-S-S-DSPE, released their contents in CFE with half-lives of 1.7 h (Fig. 3A). The release rate in CFE of the DOPE formulation with 5 mol% mPEG-S-S-DSPE was considerably slower; only 40% of encapsulated dye was released over 24 h (Fig. 3A). All three DOPE/CHEMS formulations, with or without mPEG-S-S-DSPE, released HPTS rapidly in CFE at pH 5.5; this release was almost complete by 8 h (Fig. 3B). DOPE/CHEMS and DOPE/CHEMS/mPEG-S-S-DSPE formulations incubated in CFE adjusted to pH 7.4 released HPTS at much slower rates (data not shown).

由于CFE预计含有细胞质和溶酶体酶，亲水性、膜不可渗透的染料HPTS从暴露于CFE的制剂中泄漏可能会模拟用mPEG-DSPE或mPEG-S-S-DSPE稳定的脂质体在细胞内环境中的失稳过程。

将CFE调节至pH 5.5，使溶酶体pH值接近5至6.5。DOPE制剂或含有3 mol%mPEG-S-S-DSPE的DOPE制剂在CFE中释放其含量，半衰期为1.7小时。

含有5mol%mPEG-S-S-DSPE的DOPE制剂在CFE中的释放速率明显较慢；24小时内仅释放了40%的包封染料。所有三种DOPE/CHEMS制剂，无论是否含有mPEG-S-S-DSPE，在pH 5.5的CFE中都能快速释放HPTS；8小时后，释放几乎完成。在pH 7.4的CFE中孵育的DOPE/CHEMS和DOPE/CHEMS/mPEG-S-S-DSPE制剂以慢得多的速率释放HPTS。

相关推荐：

CLS-PEG-Mal

CLS-PEG-FA

CLS-PEG-SH

CLS-PEG-NH2

CLS-PEG-COOH

CLS-PEG-SC

mPEG-CLS

8-ArmPEG-CLS

4-ARMPEG-CLS

CLS-PEG-CLS

CY7-PEG-DSPE

Galactose-PEG-Palmitic acid

以上文章内容来源各类期刊或文献，如有侵权请联系我们删除！