基于树状大分子的SPECT成像造影剂的构建及其应用  

Construction and Application of Dendrimer-Based SPECT Imaging Agent

作　　者：赵平平 杨军星 施健辉 朱静怡 Pingping Zhao;Junxing Yang;Jianhui Shi;Jingyi Zhu(School of Pharmaceutical Sciences,Nanjing Tech University,Nanjing 211800,China)

机构地区：[1]南京工业大学药学院,南京211800

出　　处：《化学进展》2021年第3期394-405,共12页Progress in Chemistry

基　　金：国家自然科学基金项目(No.21807059);江苏省自然科学基金项目(No.BK20180711);江苏省高等学校自然科学研究面上项目(No.17KJB350005);江苏省研究生科研与实践创新计划项目(KYCX201122)资助

摘　　要：树状大分子具有精准的化学结构,包括小分子内核、多分枝形成的内部空腔以及表面大量的官能团,可用于负载多种纳米颗粒及进行功能化修饰。此外,基于树状大分子的优异性能,具有良好的生物相容性及稳定性,经过功能化修饰后,其可在体内实现较长时间的血液循环和较高的组织特异性。因此,近年来常将树状大分子作为构建SPECT成像造影剂的理想载体使用。通过不同功能基团修饰树状大分子,降低纳米载体的细胞毒性,提高肿瘤部位的富集等,以实现精准高效的SPECT成像。SPECT成像主要通过监测放射性核素的体内分布、流动及代谢情况以在分子层面上监测病灶部位的生理、病理学变化。相比于小分子的放射性核素,以树状大分子为载体构建的SPECT成像造影剂体内循环时间更长,且经过功能化修饰后可实现体内特异性分布。本文围绕各类放射性核素标记的功能化树状大分子进行了详细阐述,并总结归纳其制备方法及生物医学应用。最后,对这类基于树状大分子的SPECT成像造影剂在肿瘤早期诊断中的应用前景进行了展望。Dendrimer owns a precise chemical structure,including a small molecular core,an internal space induced by multiple branches,and large numbers of functional groups on the surface,which can be used to load a variety of nanoparticles and perform functional modification.In addition,based on the excellent properties of dendrimer,it demonstrates good biocompatibility and stability.After functional modification,it could achieve long blood circulation and high tissue specificity in vivo.Therefore,dendrimer has often been used as an ideal carrier for constructing SPECT imaging agents in recent years.Through multifunctional modification with various functional groups,the cytotoxicity of the generated nanocarrier is decreased and its accumulation at tumor site is improved,which faciliates accurate and efficient SPECT imaging.SPECT imaging monitors the physiological and pathological changes of lesions at the molecular level via monitoring the distribution,flow and metabolism of radionuclides in vivo.Compared with small molecular radionuclides,dendrimer-based SPECT imaging agents demonstrate longer circulation time and could achieve specific distribution after functional modification in vivo.In this review,various radionuclides labeled functional dendrimers are described in detail,their preparation methods and biomedical applications are summarized.Finally,the applications of these dendrimer-based SPECT imaging agents in the early diagnosis of tumor are prospected.

关 键 词：分子影像学 纳米造影剂 树状大分子 SPECT成像 生物医学应用 

分 类 号：O63[理学—高分子化学] TL923[理学—化学]