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In this review, we classify strategies into five complementary directions: (i) TME remodeling/barrier relief, (ii) size and charge transformation, (iii) ligand- and ligand-guided transcytosis driven by the C-end Rule (CendR) motif through neuropilin-1 (NRP1)-guided transcytosis, (iv) cell-based and bioinspired carriers (including cell-penetrating peptide (CPP) modules), and (v) multistage cascade systems (Fig