(A) A dual-targeting delivery liposomal system was designed with dual-modification of PD-L1 nanobody and mannose ligands for co-delivering an mTOR inhibitor (rapamycin) and an anti-angiogenic drug (regorafenib). The liposomes were able to target both TAMs and cancer cells that overexpressed PD-L1 and mannose receptors, and then efficiently reduced glycolysis, repolarized TAMs, inhibited angiogenesis, reprogrammed immune cells, and consequently arrested tumor growth. Adapted with permission from 133, copyright 2020 Elsevier Ltd. (B) Schematic illustration of the enhanced cancer chemo-immunotherapy resulting from intratumorally and intravenously injected nanomedicines. Of which, the immunostimulatory micelle ACP-R837 activated TAMs and promoted the secretion of cytokines, leading to an augmented antitumor immune response. Adapted with permission from 96, copyright 2019 Elsevier Ltd. (C) Schematic illustration of the formation of R848-loaded PLGA NP coated with E. coli (Ec-PR848) and TAMs re-polarization-promoted cancer immunotherapy. (D) Flow cytometric analysis of the proportion of M1 macrophages (F4/80+CD80+) and M2 macrophages (F4/80+CD206+). Adapted with permission from 148, copyright 2021 American Chemical Society. Abbreviations: mTOR: mammalian target of rapamycin; GZMB: granzyme B; TLR-7: toll-like receptor 7; i.t.: intratumoral; i.v.: intravenous.