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：

radiolabeled [125I]TI were prepared and injected into the tail vein of mice at a PL dose of 0.5 μmol/mouse. Circulation times increased with increasing concentration of mPEG-DSPE in either DOPE or DOPE/CHEMS liposome formulations (Fig. 6A,B). Approximately 5–10% of the injected liposomes still remained in the blood 24 h after injection of liposomes containing 10 mol% mPEG-DSPE. Injection of DOPE or DOPE/CHEMS liposomes that were not stabilized with mPEG-DSPE resulted in rapid clearance of the liposomes. Liposomes accumulated primarily in the liver and spleen (not shown). Inclusion of from 2 to 9 mol% of mPEG-S-S-DSPE did not increase the circulation times for either the DOPE (Fig. 6C) or DOPE/CHEMS (Fig. 6D) formulations. All mPEG-S-S-DSPE formulations contained 1 mol% mPEG-DSPE to mimic the effect of adding 1 mol% coupling lipid to the formulations in targeting experiments. Increasing amounts of mPEG-S-S-DSPE in the formulations did not increase circulation half-lives of the formulations to any significant extent (Fig. 6A,B), likely because the mPEG-S-S-DSPE was rapidly cleaved in plasma.



为了确定脂质体制剂的药代动力学，制备了含有放射性标记的[125I]TI的脂质体，并以0.5μmol/小鼠的PL剂量注射到小鼠的尾静脉中。循环时间随着DOPE或DOPE/CHEMS脂质体制剂中mPEG-DSPE浓度的增加而增加。

注射含有10mol%mPEG-DSPE的脂质体24小时后，约5-10%的注射脂质体仍留在血液中。注射未经mPEG-DSPE稳定的DOPE或DOPE/CHEMS脂质体可快速清除脂质体。脂质体主要积聚在肝脏和脾脏中。

加入2至9mol%的mPEG-S-S-DSPE不会增加DOPE或DOPE/CHEMS制剂的循环时间。所有mPEG-S-S-DSPE制剂均含有1 mol%mPEG-DSPE，以模拟在靶向实验中向制剂中添加1 mol%偶联脂质的效果。制剂中mPEG-S-S-DSPE含量的增加并没有显著延长制剂的循环半衰期，这可能是因为mPEG-S-S-D SPE在血浆中迅速裂解。

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