Nickels Michael, Xie Jingping, Cobb Jared, Gore John C, Pham Wellington
Vanderbilt University, Institute of Imaging Science, 1161 21 Avenue South, AA 1105 MCN, Nashville, TN, 37232-2310, USA.
J Mater Chem. 2010;20(23):4776-4780. doi: 10.1039/c0jm00808g.
A synthetically diverse linker molecule consisting of both a terminal epoxide and a terminal amine has been synthesized and shown to have the desired reactivity. Proof of principle experimentation showed that the prepared linker molecule possessed the ability to be reactive towards dextran coated iron nanoparticles, essentially converting the surface alcohols to amines with an efficiency on average of 50 linkers per nanoparticle. Once the surface of the nanoparticles had been functionalized, the iron nanoparticles were subsequently functionalized with both folic acid and fluorescein isothiocyanate, with an average efficiency of 20 and 3 molecules per nanoparticle, respectively. The labeled nanoparticles were then incubated with both folate receptor positive and negative cell lines, which showed a preferential accumulation of the particles in the receptor positive cell line. In addition to the fluorescence based assays, accumulation of the nanoparticles was demonstrated using T2-weighted MRI imaging, which showed that the iron core of the nanoparticle was present within the desired cell line. Overall, this linker has shown the ability to functionalize the surface of nanoparticles and can theoretically be used to label a wide variety of other targeting agents or imaging agents for in vivo therapies or diagnostics.
一种由末端环氧化物和末端胺组成的具有合成多样性的连接分子已被合成，并显示出具有所需的反应活性。原理验证实验表明，所制备的连接分子具有与葡聚糖包被的铁纳米颗粒发生反应的能力，基本上能将表面醇转化为胺，平均每个纳米颗粒有50个连接分子的转化效率。一旦纳米颗粒表面被功能化，铁纳米颗粒随后分别用叶酸和异硫氰酸荧光素进行功能化，平均每个纳米颗粒的效率分别为20个和3个分子。然后将标记的纳米颗粒与叶酸受体阳性和阴性细胞系一起孵育，结果显示颗粒在受体阳性细胞系中优先积累。除了基于荧光的检测方法外，还使用T2加权磁共振成像证明了纳米颗粒的积累，该成像显示纳米颗粒的铁芯存在于所需的细胞系中。总体而言，这种连接分子已显示出能够使纳米颗粒表面功能化，并且理论上可用于标记多种其他靶向剂或成像剂，用于体内治疗或诊断。
