Owing to the unique structural characteristics and abundant amine groups, polyethylenimine (PEI) plays a remarkable role in the construction of multifunctional nanosystems for versatile biomedical applications, particular for cancer nanomedicine. Nanoparticles (NPs), polymers, fluorophores, targeting molecules or/and different cargos can be integrated within one single system via PEI-mediated chemistry, thereby allowing for the generation of a range of PEI-based nanoplatforms. On the molecular imaging front, PEI-based NPs serve as contrast agents to transduce biomolecular interactions into various types of signals for single-, dual- or multi-mode imaging of tissues and diseases. With rational modifications, PEI-based nanocarriers can be developed and utilized for targeted and responsive delivery of drugs, genes and proteins. Utilizing the unique features of PEI-based NPs that can convert external stimuli (e.g., magnetic field, light and X-ray) into heat or free radical, in vivo magnetic hyperthermia, phototherapy, and radiotherapy can be realized, achieving excellent anti-tumor therapeutic outcomes. In this review, we summarize the recent progress in the development of PEI-based multifunctional nanosystems for versatile biomedical applications in cancer nanomedicine and discuss the current challenges and future prospects in this related field.

由于独特的结构特征和丰富的胺基团，聚乙烯亚胺（PEI）在构建多功能纳米系统用于多功能生物医学应用方面发挥着显着的作用，尤其是在癌症纳米医学方面。纳米颗粒（NP），聚合物，荧光团，靶向分子或/和不同货物可以在一个单一的系统中被集成经由PEI 介导的化学，从而允许生成一系列基于 PEI 的纳米平台。在分子成像方面，基于 PEI 的 NP 作为造影剂将生物分子相互作用转换为各种类型的信号，用于组织和疾病的单、双或多模式成像。通过合理的修改，基于 PEI 的纳米载体可以被开发和用于药物、基因和蛋白质的靶向和响应性递送。利用基于 PEI 的 NPs 的独特功能，可以在体内将外部刺激（例如磁场、光和 X 射线）转化为热量或自由基可实现磁热疗、光疗、放疗，取得优异的抗肿瘤治疗效果。在这篇综述中，我们总结了基于 PEI 的多功能纳米系统在癌症纳米医学中的多功能生物医学应用的最新进展，并讨论了该相关领域的当前挑战和未来前景。