Macrophages have a leading position in the tumor microenvironment (TME) which paves the way to carcinogenesis. Initially, monocytes and macrophages are recruited to the sites where the tumor develops. Under the guidance of different microenvironmental signals, macrophages would polarize into two functional phenotypes, named as classically activated macrophages (M1) and alternatively activated macrophages (M2). Contrary to the anti-tumor effect of M1, M2 exerts anti-inflammatory and tumorigenic characters. In progressive tumor, M2 tumor-associated macrophages (TAMs) are in the majority, being vital regulators reacting upon TME. This review elaborates on the role of TAMs in tumor progression. Furthermore, prospective macrophage-focused therapeutic strategies, including drugs not only in clinical trials but also at primary research stages, are summarized followed by a discussion about their clinical application values. Nanoparticulate systems with efficient drug delivery and improved antitumor effect are also summed up in this article.

巨噬细胞在肿瘤微环境（TME）中具有领先地位，为致癌作用铺平了道路。最初，单核细胞和巨噬细胞被募集到肿瘤发生的部位。在不同的微环境信号的指导下，巨噬细胞将极化为两种功能表型，分别称为经典活化的巨噬细胞（M1）和交替活化的巨噬细胞（M2）。与M1的抗肿瘤作用相反，M2具有抗炎和致瘤性。在进行性肿瘤中，M2肿瘤相关巨噬细胞（TAM）占多数，是对TME产生反应的重要调节剂。这篇综述详细阐述了TAM在肿瘤进展中的作用。此外，针对巨噬细胞的前瞻性治疗策略，不仅包括临床试验中的药物，还包括初级研究阶段的药物，总结，然后讨论其临床应用价值。本文还总结了具有有效药物输送和改善的抗肿瘤作用的纳米颗粒系统。