State Key Laboratory of Rare Earth Resources Utilization and Laboratory of Chemical Biology, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, PR China.
Biomaterials. 2012 Oct;33(28):6748-57. doi: 10.1016/j.biomaterials.2012.06.033. Epub 2012 Jul 6.
Nanoparticulate imaging agents offer excellent diagnostic and therapeutic capabilities due to their intense and stable output, strong target binding via multiple ligands, as well as tunable biodistribution profiles. In the present work, we designed and synthesized PEGylated Yb(2)O(3):Er nanoparticles with high Yb content in single particle (denoted as PEG-UCNPs) suitable for both X-ray CT imaging and up-conversion imaging. These PEG-UCNPs were facile to construct, possessed excellent stability against in vivo environment, and held long blood circulation time. Cell-cytotoxicity assay, hemolyticity, and post-injection histology analysis further demonstrated the excellent biocompatibility, indicating the feasibilities of PEG-UCNPs for in vivo applications. Compared with routinely used Iobitridol in clinic, well-prepared PEG-UCNPs provided much significantly enhanced contrast at a clinical 120 kVp voltage. By doping 5% Er(3+) into the nanoparticles, PEG-UCNPs presented a long-term stable and nearly single-band red up-conversion emission upon continuous irradiation with an assistant of a 980 laser. In addition, pharmacokinetics, biodistribution, as well as clearance of nanoparticles were studied after intravenous injection in a mouse model, reflecting their overall safety. PEG-UCNPs composed of intrinsic up-conversion luminescence property, higher X-ray absorption over Iobitridol, as well as excellent biocompatibility represented a nanoplatform for biomedicine applications.
纳米颗粒成像剂由于其高强度和稳定的输出、通过多个配体的强靶结合以及可调的生物分布特性，提供了出色的诊断和治疗能力。在本工作中，我们设计并合成了具有高单颗粒 Yb 含量的聚乙二醇化 Yb(2)O(3):Er 纳米颗粒（表示为 PEG-UCNPs），适合 X 射线 CT 成像和上转换成像。这些 PEG-UCNPs 易于构建，对体内环境具有优异的稳定性，并且具有较长的血液循环时间。细胞毒性试验、溶血试验和注射后组织学分析进一步证明了其优异的生物相容性，表明 PEG-UCNPs 适用于体内应用。与临床上常用的碘比醇相比，精心制备的 PEG-UCNPs 在临床 120kVp 电压下提供了明显更高的对比度。通过在纳米颗粒中掺杂 5%的 Er(3+)，PEG-UCNPs 在 980nm 激光的辅助下，可实现长期稳定且几乎单波段的红色上转换发射。此外，还研究了纳米颗粒在小鼠模型中的药代动力学、生物分布和清除情况，反映了其整体安全性。PEG-UCNPs 具有内在的上转换发光特性、比碘比醇更高的 X 射线吸收以及优异的生物相容性，代表了一种用于生物医学应用的纳米平台。
