Acid-triggered transformation of diortho ester phosphocholine liposome
Acid-triggered transformation of diortho ester phosphocholine liposome
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DOI：
10.1021/ja057024w
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发表时间：
2006-01-11
影响因子：
15
通讯作者：
Szoka, FC
中科院分区：
文献类型：
--
作者：
Huang, ZH;Guo, X;Szoka, FC
利用pH敏感脂质体进行酸触发定点给药是提高药物治疗指数的最有前途的方法之一。在这里，我们报告的合成，组装和水解的第一个原酸酯磷酸胆碱（OEPC）。OEPC脂质体的酸水解包括滞后期和爆发期。滞后时间取决于pH值-pH值越低，时间越短。在酸水解后，OEPC脂质体转化为在白蛋白存在下快速塌陷的渗漏亚稳囊泡。与pH不敏感的制剂相比，当与阳离子脂质一起配制时，OEPC显著增强了转染效率。
The use of pH-sensitive liposomes for acid-triggered site-specific drug delivery is one of the more promising approaches to improve the therapeutic index of drugs. Here, we report the synthesis, assembly, and hydrolysis of the first ortho ester phosphocholine (OEPC). The acid hydrolysis of OEPC liposomes consists of a lag phase and a burst phase. The lag time is pH-dependent—the lower the pH, the shorter the time. Upon acid hydrolysis, the OEPC liposomes were transformed into leaky metastable vesicles that rapidly collapsed in the presence of albumin. OEPC, when formulated with cationic lipid, significantly enhanced the transfection efficiency compared with that of the pH-insensitive formulation.