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聚乙二醇-脂质衍生物修饰对脂质体稳定性的影响
引用本文:Xu Y,Shi L,Deng YH. 聚乙二醇-脂质衍生物修饰对脂质体稳定性的影响[J]. 药学学报, 2011, 46(10): 1178-1186
作者姓名:Xu Y  Shi L  Deng YH
作者单位:沈阳药科大学药学院;辽宁省药物研究院;
基金项目:国家自然科学基金资助项目(81072602)
摘    要:聚乙二醇-脂质(polyethylene glycol-lipid,PEG-lipid)衍生物具有增加脂质体的稳定性、延长其血液循环半衰期、提高其肿瘤靶向效率及增强药物疗效等优势。深入研究不同PEG-lipid衍生物修饰对脂质体的物理、化学和生物学稳定性的影响,有利于解决目前PEG化脂质体存在的问题,如静脉重复注射时引起的加速血液消除(accelerated blood clearance,ABC)现象,为开发新型靶向制剂奠定基础。本文主要综述了PEG与脂质之间的连接键如酰胺键、醚键、酯键和二硫键,脂质种类如常用的磷脂酰乙醇胺、胆固醇和二酰甘油,脂质的性质即脂肪链长度与饱和度,PEG的端基如甲氧基、羧基、氨基,PEG的相对分子质量和PEG-lipid的摩尔比对PEG化脂质体在体内外稳定性的影响。

关 键 词:聚乙二醇-脂质衍生物  脂质体  稳定性  

Effect of polyethylene glycol-lipid derivatives on the stability of grafted liposomes
Xu Yang,Shi Li,Deng Yi-hui. Effect of polyethylene glycol-lipid derivatives on the stability of grafted liposomes[J]. Acta pharmaceutica Sinica, 2011, 46(10): 1178-1186
Authors:Xu Yang  Shi Li  Deng Yi-hui
Affiliation:XU Yang1,SHI Li2,DENG Yi-hui1(1.School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China,2.Liaoning Institute of Pharmaceutical Industry,Shenyang 110015,China)
Abstract:It is reported that polyethylene glycol-lipid(PEG-lipid) derivatives increase liposomes stability,prolong the blood circulation of liposomes,enhance their tumor-targeting efficiency,and improve drug efficacy.Therefore,it is of great importance to investigate the influence of modified PEG-lipid derivatives on the physical,chemical,and biological characteristics of liposomes for the promotion of dealing with the existed problems,such as the accelerated blood clearance(ABC) phenomenon when repeated intravous i...
Keywords:PEG-lipid derivative  liposome  stability  
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