文獻(xiàn)：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 

文獻(xiàn)鏈接：

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.

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為了確定脂質(zhì)體制劑的藥代動(dòng)力學(xué)，制備了含有放射性標(biāo)記的[125I]TI的脂質(zhì)體，并以0.5μmol/小鼠的PL劑量注射到小鼠的尾靜脈中。循環(huán)時(shí)間隨著DOPE或DOPE/CHEMS脂質(zhì)體制劑中mPEG-DSPE濃度的增加而增加。

注射含有10mol%mPEG-DSPE的脂質(zhì)體24小時(shí)后，約5-10%的注射脂質(zhì)體仍留在血液中。注射未經(jīng)mPEG-DSPE穩(wěn)定的DOPE或DOPE/CHEMS脂質(zhì)體可快速清除脂質(zhì)體。脂質(zhì)體主要積聚在肝臟和脾臟中。

加入2至9mol%的mPEG-S-S-DSPE不會(huì)增加DOPE或DOPE/CHEMS制劑的循環(huán)時(shí)間。所有mPEG-S-S-DSPE制劑均含有1 mol%mPEG-DSPE，以模擬在靶向?qū)嶒?yàn)中向制劑中添加1 mol%偶聯(lián)脂質(zhì)的效果。制劑中mPEG-S-S-DSPE含量的增加并沒有顯著延長(zhǎng)制劑的循環(huán)半衰期，這可能是因?yàn)閙PEG-S-S-D SPE在血漿中迅速裂解。

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