The architecture of ligand attachment to nanocarriers controls their specific interaction with target cells.
The architecture of ligand attachment to nanocarriers controls their specific interaction with target cells.
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DOI：
10.1080/10611860802230240
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发表时间：
2008-08
影响因子：
4.5
通讯作者：
Torchilin VP
中科院分区：
文献类型：
--
作者：
Sawant RR;Sawant RM;Kale AA;Torchilin VP
药物纳米载体的表面结构（使用聚合物胶束作为实例）和间隔基团的长度决定了携带配体的纳米载体与细胞的相互作用，特异性配体通过所述间隔基团连接到载体表面。我们制备了表面改性的聚乙二醇-磷脂酰乙醇胺（PEG-PE）胶束，其含有连接到PEG-PE上的TATp，其中PEG嵌段（TATp-PEG 1000-PE或TATp-PEG 3400-PE）比主要胶束形成材料（PEG 750-PE和/或PEG 2000-PE）中的PEG嵌段更长或更短。TATp-PEG-PE中PEG间隔基的长度应允许TATp与细胞表面的无阻碍相互作用，但其不应太长以允许PEG球内的TATp部分的构象“折叠”，使其不能与细胞相互作用。通过荧光标记的脂质1，2-二棕榈酰-sn-甘油基-3-磷酸乙醇胺-N-（7-硝基-2-1，3-苯并恶二唑-4-基）（NBD-PE）插入PEG 750-PE胶束的核心和胶束掺入的罗丹明标记的TAT p-PEG-PE之间的荧光共振能量转移（FRET）研究，进一步支持了连接到不必要的长PEG间隔基的配体的“折叠”。含有具有最长PEG间隔基（3400 Da）的罗丹明标记的TATp-PEG-PE的胶束证明了用罗丹明-TATp强烈增强的NBD-PE荧光猝灭，证实了TATp部分“折叠”到PEG球中，使其更接近胶束核并入的NBD。
Surface architecture of pharmaceutical nanocarriers (using polymeric micelles as an example) and the length of the spacer group through which specific ligand is attached to the carrier surface determine the interaction of ligand-bearing nanocarrier with cells. We have prepared surface-modified polyethyleneglycol–phosphatidylethanolamine (PEG–PE) micelles containing TATp attached to PEG–PE with a PEG block longer or shorter (TATp–PEG1000–PE or TATp–PEG3400–PE) than the PEG block in the main micelle-forming material (PEG750–PE and/or PEG2000–PE). The length of the PEG spacer in TATp–PEG–PE should allow for a non-hindered interaction of TATp with the cell surface, but it should not be too long to allow for the conformational “folding in” of TATp moiety inside the PEG globule making it unable to interact with the cells. The “folding in” of the ligand attached to an unnecessary long PEG spacer was further supported by the fluorescence resonance energy transfer (FRET) study between fluorescently labeled lipid 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine-N-(7-nitro-2-1,3-benzoxadiazol-4-yl) (NBD-PE) inserted into the core of PEG750–PE micelles and micelle-incorporated rhodamine-labeled TATp–PEG–PE. Micelles containing rhodamine-labeled TATp–PEG–PE with the longest PEG spacer (3400 Da) demonstrated strongly enhanced quenching of NBD-PE fluorescence with rhodamine-TATp confirming the “folding in” of TATp moiety into PEG globule bringing it closer to the micelle core-incorporated NBD.
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影响因子：
2.2
作者：
Dodd, CH;Hsu, HC;Mountz, JD
通讯作者：
Mountz, JD
影响因子：
10.8
作者：
Kleemann, E;Neu, M;Kissel, T
通讯作者：
Kissel, T
影响因子：
4.7
作者：
Sawant, R. M.;Hurley, J. P.;Torchilin, V. P.
通讯作者：
Torchilin, V. P.
影响因子：
10.8
作者：
Hyndman, L;Lemoine, JL;Nan, XS
通讯作者：
Nan, XS
影响因子：
3
作者：
Nitin, N;LaConte, LEW;Bao, G
通讯作者：
Bao, G