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基于mPEG-DSPE与CHEMS-PEG构建的囊泡系统性能研究
发布时间:2025-07-10     作者:zyl   分享到:
期刊论文:Esterase-catalyzed dePEGylation of pH-sensitive vesicles modified with cleavable PEG-lipid derivatives小编:Huan Xu a b, Yihui Deng a, Dawei Chen a, Weiwei Hong a, Yi Lu a, Xiaohui Dong 医学文献超链接:


To make vesicles for the better controlled content release, we modified cholesteryl hemisuccinate (CHEMS)-derived vesicles with PEG-lipid derivatives. Two cholesterol analogs, cholesteryl hemisuccinate (CHEMS) and cholesteryl chloroformate (CHM), have been conjugated to the polyethylene glycol (PEG) via their ester bonds for the vesicle modifications, so the PEGs can be cleaved by esterases. The effects of PEG-lipid proportions, serum concentrations and the lipid types on the esterase-catalyzed cleavage of PEG polymer off the vesicles surface were determined. We observed that PEG cleavages decreased as the molar ratios of the PEG-lipids in vesicles increased; on the other hand, PEG cleavages gradually increased with the increased serum concentrations. In contrast to conventional long circulation materials mPEG-DSPE and mPEG-CHOL, the two new conjugates enabled higher degrees of PEG cleavages from modified vesicles. After incubation in the serum at acidic conditions, esterase-catalyzed dePEGylation destabilized these vesicles, increasing the mean particle sizes and promoting content releases. These results suggested that ester linkages between the PEG and lipid anchors allow faster content releases in the suitable conditions. Together, the two esterase cleavable PEG-lipid conjugations may be applied not only to stabilize vesicles and prolong their circulation time, but also to provide more efficient content releases by the esterase controlled dePEGylation.

mPEG-DSPE

从而提纯更稳地调节信息物减少的囊泡,大家用PEG脂质并产生物装饰了高密度脂蛋白升高升高升高半蜜腊酸盐(CHEMS)并产生的囊泡。不同高密度脂蛋白升高升高升高近似物,高密度脂蛋白升高升高升高半蜜腊酸酯(CHEMS)和高密度脂蛋白升高升高升高氯甲酸酯(CHM),能能通过其酯键与聚乙二醇(PEG)组合完成囊泡装饰,因而PEG能能被酯酶分割。测得了PEG脂质标准、血清氧化还原电位和脂质类形对酯酶催化剂的作用PEG缔合物从囊泡外面打磨的决定。当我们关察到,日渐囊泡中PEG脂质摩尔比的增高,PEG裂解减轻;另外一只工作方面,PEG裂解日渐血清氧化还原电位的增高而日渐增高。与中国传统的长再循环板材mPEG-DSPE和mPEG-CHOL较之,这五种新的偶联物就能从装饰的囊泡中体现更快方面的PEG裂解。在呈酸性条件下到血清中孵育后,酯酶促使的去聚乙二醇化使以下囊泡失稳,上升了均衡孔径并利于了信息物的缓解压力。这种结论表述,PEG和脂质锚中间的酯键在适合的的必要条件下充许快速的知识物发出。这二种酯酶可裁切的PEG-脂质偶联物还能否一个软件,不禁还能否维持囊泡并调长其不断循环時间,还还能否经由酯酶操作的去聚乙二醇化带来了更管用的知识物发出。关于安利:C18-PEGn-OPSSC18-PEGn-SH (SH: Thiol)mPEG-Cholesterol (mPEG-CLS)mPEG-CONH-C12mPEG-CONH-C16mPEG-CONH-C18mPEG-DMPEmPEG-DSPEmPEG-O-C12mPEG-O-C16mPEG-O-C18mPEG-Unsaturated Fatty Acid之内稿件玩法来自各期刊论文或医学文献,如不商标侵权请链接我们大家删掉!