School of Life Sciences, East China Normal University, Shanghai, 200062, People's Republic of China.
Chem Soc Rev. 2011 May;40(5):2673-703. doi: 10.1039/c0cs00097c. Epub 2011 Feb 1.
In the past decade, nanomedicine with its promise of improved therapy and diagnostics has revolutionized conventional health care and medical technology. Dendrimers and dendrimer-based therapeutics are outstanding candidates in this exciting field as more and more biological systems have benefited from these starburst molecules. Anticancer agents can be either encapsulated in or conjugated to dendrimer and be delivered to the tumour via enhanced permeability and retention (EPR) effect of the nanoparticle and/or with the help of a targeting moiety such as antibody, peptides, vitamins, and hormones. Imaging agents including MRI contrast agents, radionuclide probes, computed tomography contrast agents, and fluorescent dyes are combined with the multifunctional nanomedicine for targeted therapy with simultaneous cancer diagnosis. However, an important question reported with dendrimer-based therapeutics as well as other nanomedicines to date is the long-term viability and biocompatibility of the nanotherapeutics. This critical review focuses on the design of biocompatible dendrimers for cancer diagnosis and therapy. The biocompatibility aspects of dendrimers such as nanotoxicity, long-term circulation, and degradation are discussed. The construction of novel dendrimers with biocompatible components, and the surface modification of commercially available dendrimers by PEGylation, acetylation, glycosylation, and amino acid functionalization have been proposed as available strategies to solve the safety problem of dendrimer-based nanotherapeutics. Also, exciting opportunities and challenges on the development of dendrimer-based nanoplatforms for targeted cancer diagnosis and therapy are reviewed (404 references).
在过去的十年中，纳米医学以其改善治疗和诊断的承诺，彻底改变了传统的医疗保健和医疗技术。树状大分子和基于树状大分子的治疗剂是这一令人兴奋的领域中的杰出候选者，因为越来越多的生物系统受益于这些星爆分子。抗癌剂可以被包裹在或连接到树状大分子上，并通过纳米颗粒的增强渗透性和保留（EPR）效应和/或借助靶向部分（如抗体、肽、维生素和激素）递送到肿瘤部位。成像剂，包括 MRI 造影剂、放射性核素探针、计算机断层扫描造影剂和荧光染料，与多功能纳米医学结合，用于靶向治疗和同时进行癌症诊断。然而，一个重要的问题是，基于树状大分子的治疗剂以及迄今为止的其他纳米医学，是纳米治疗剂的长期生存能力和生物相容性。本综述重点介绍了用于癌症诊断和治疗的生物相容树状大分子的设计。讨论了树状大分子的生物相容性方面，如纳米毒性、长期循环和降解。通过使用生物相容成分构建新型树状大分子，以及通过 PEG 化、乙酰化、糖基化和氨基酸功能化对市售树状大分子进行表面修饰，已被提出作为解决基于树状大分子的纳米治疗剂安全性问题的可行策略。此外，还回顾了基于树状大分子的纳米平台在靶向癌症诊断和治疗方面的发展所带来的令人兴奋的机遇和挑战（404 篇参考文献）。
