Surface-engineered nanoparticles for multiple ligand coupling
Surface-engineered nanoparticles for multiple ligand coupling
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DOI：
10.1016/s0142-9612(03)00348-x
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发表时间：
2003-11-01
期刊：
影响因子：
14
通讯作者：
Mysiakine, E
中科院分区：
文献类型：
--
作者：
Gref, R;Couvreur, P;Mysiakine, E
设计用于靶向特定位点的表面工程纳米颗粒是一个重大挑战。据我们所知，文献中没有研究涉及通过生物素-抗生物素蛋白相互作用使生物可降解纳米颗粒配体官能化。为了构思可以容易地用各种配体或其混合物官能化的小尺寸纳米颗粒，合成了生物素化和PEG化的生物素-聚（乙二醇）-聚（ε-己内酯）（B-PEG-PCL）共聚物，并用于制备约100 nm的纳米颗粒。利用生物素-亲和素形成强复合物的优势，将亲和素偶联到它们的表面，然后将生物素化的麦胚凝集素作为模型凝集素。纳米球对培养物中Caco-2细胞的细胞毒性可忽略不计（对于高达300 μ g/孔的纳米颗粒浓度，超过82%的细胞存活）。与Caco-2细胞相关的放射性标记的聚乳酸（PLA）或PEG-PLA纳米颗粒的量分别仅为添加量的0.7%和1.5%。当足够量的凝集素结合到PEG-PLA共聚物时，该值增加到8.5%。经过进一步的研究，生物素-PEG-包覆的纳米颗粒可以成为研究细胞与具有各种表面特征（PEG层密度和厚度，配体类型和密度）的功能化纳米颗粒之间相互作用的有用工具。(C)2003 Elsevier Ltd.保留所有权利。
The design of surface-engineered nanoparticles for targeting to specific sites is a major challenge. To our knowledge, no study in the literature deals with ligand functionalization of biodegradable nanoparticles through biotin-avidin interactions. With the aim of conceiving small-sized nanoparticles which can be easily functionalized with a variety of ligands or mixtures thereof, biotinylated and PEGylated biotin-poly(ethylene glycol)-poly(epsilon-caprolactone) (B-PEG-PCL) copolymers were synthesized and used to prepare nanoparticles of around 100 nm. Avidin, followed by biotinylated wheat germ agglutinin as a model lectin, were coupled to their surface by taking advantage of the strong biotin-avidin complex formation. The cytotoxicity of the nanospheres towards Caco-2 cells in culture was negligible (more than 82% cell survival for nanoparticle concentrations up to 300 mug/well). The amount of radiolabeled poly(lactic acid) (PLA) or PEG-PLA nanoparticles associated with Caco-2 cells was only 0.7% and 1.5% of the amount added, respectively. This value was increased to 8.5% when a sufficient amount of lectin was bound to the PEG-PLA copolymer. After further studies, the biotin-PEG-coated nanoparticles could be helpful tools for studying the interaction between cells and functionalized nanoparticles with various surface characteristics (PEG layer density and thickness, ligand type and density). (C) 2003 Elsevier Ltd. All rights reserved.