INFLUENCE OF THE STERIC BARRIER ACTIVITY OF AMPHIPATHIC POLY(ETHYLENEGLYCOL) AND GANGLIOSIDE GM1 ON THE CIRCULATION TIME OF LIPOSOMES AND ON THE TARGET BINDING OF IMMUNOLIPOSOMES INVIVO
INFLUENCE OF THE STERIC BARRIER ACTIVITY OF AMPHIPATHIC POLY(ETHYLENEGLYCOL) AND GANGLIOSIDE GM1 ON THE CIRCULATION TIME OF LIPOSOMES AND ON THE TARGET BINDING OF IMMUNOLIPOSOMES INVIVO
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DOI：
10.1016/0014-5793(91)80699-4
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发表时间：
1991-06-24
期刊：
影响因子：
3.5
通讯作者：
HUANG, L
中科院分区：
文献类型：
--
作者：
MORI, A;KLIBANOV, AL;HUANG, L
本研究使用了一系列不同聚合物链长的二油酰N-(单甲氧基聚乙二醇琥珀酰)磷脂酰乙醇胺(PEG-PE)。通过脂质体凝集测定测定，PEG-PE 延长脂质体循环时间的活性和两亲性聚合物的相对空间屏障活性均与 PEG-PE 的链长成正比（PEG5000-PE > PEG2000-PE > PEG750-PE）。然而，PEG5000-PE由于其过强的空间屏障活性导致小鼠免疫脂质体的靶标结合减少。支持免疫脂质体靶向结合的最佳PEG-PE种类是PEG2000-PE，其活性与神经节苷脂GM1的活性相容。然而，GM1 仅表现出较弱的空间屏障活性，表明该糖脂具有不同的机制。
A series of dioleoyl N-(monomethoxy polyethyleneglycol succinyl)phosphatidylethanolamine (PEG-PE) of different polymer chain length was used in this study. Both the activity of PEG-PE in prolonging the circulation time of liposomes and the relative steric barrier activity of amphipathic polymer, measured by a liposome agglutination assay, were found to be directly proportional to the chain length of PEG-PE (PEG5000-PE > PEG2000-PE > PEG750-PE). However, PEG5000-PE caused a reduced target binding of immunoliposomes in mice due to its overly strong steric barrier activity. The best PEG-PE species supporting the target binding of immunoliposomes was PEG2000-PE, the activity of which was compatible to that of ganglioside GM1. However, GM1 only showed a weak steric barrier activity, suggesting a different mechanism for this glycolipid.