Chen F H, Gao Q, Ni J Z
State Key Laboratory of Rare Earth Resources and Application, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, People's Republic of China. Graduate University of the Chinese Academy of Sciences, Beijing 100049, People's Republic of China.
Nanotechnology. 2008 Apr 23;19(16):165103. doi: 10.1088/0957-4484/19/16/165103. Epub 2008 Mar 18.
Fe(3)O(4)@SiO(2) core-shell structure nanoparticles were first prepared and characterized by TEM, FTIR, XPS and XRD. Subsequently the widely used anticancer agent doxorubincin (DOX) was successfully grafted to the surface of the core-shell nanoparticles via an amide bond with the aid of a spacer arm we synthesized. The spacer arm met two needs: one end can couple to the core-shell nanoparticles' surface while the other end was the active -COOH group, which can react with the -NH(2) group of DOX molecules. The synthesized spacer arm and the conjugation of the drug with nanoparticles through amidation were confirmed by FTIR. The DOX-loading efficiency determined by UV-vis spectrometer was 86.5%. Drug release experiments displayed a pH-dependent behavior that DOX was cleaved from the nanoparticles easily under low pH conditions in the presence of protease and that most of the conjugated doxorubincin were released within the first 12 h. The prepared DOX-grafted Fe(3)O(4)@SiO(2) core-shell structure nanoparticles showed a superparamagnetic property with a saturation magnetization value of 49.3 emu g(-1), indicating a great potential application in the treatment of cancer using magnetic targeting drug-delivery technology.
首先制备了Fe(3)O(4)@SiO(2)核壳结构纳米颗粒，并通过透射电子显微镜（TEM）、傅里叶变换红外光谱（FTIR）、X射线光电子能谱（XPS）和X射线衍射（XRD）对其进行了表征。随后，在我们合成的间隔臂的帮助下，通过酰胺键成功地将广泛使用的抗癌药物阿霉素（DOX）接枝到核壳纳米颗粒的表面。间隔臂满足了两个需求：一端可以与核壳纳米颗粒的表面偶联，而另一端是活性-COOH基团，其可以与DOX分子的-NH(2)基团反应。通过FTIR证实了合成的间隔臂以及药物通过酰胺化与纳米颗粒的缀合。通过紫外可见光谱仪测定的DOX负载效率为86.5%。药物释放实验显示出pH依赖性行为，即在低pH条件下，在蛋白酶存在的情况下，DOX很容易从纳米颗粒上裂解下来，并且大多数缀合的阿霉素在最初的12小时内释放。制备的接枝DOX的Fe(3)O(4)@SiO(2)核壳结构纳米颗粒表现出超顺磁性，饱和磁化强度值为49.3 emu g(-1)，表明在使用磁靶向药物递送技术治疗癌症方面具有巨大的潜在应用。
