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Tumor cell targeting of drug carriers is a promising strategy and uses the attachment of various ligands to enhance the therapeutic potential of chemotherapy agents. Folic acid is a high‐affinity ligand for folate receptor, which is a functional tumor‐specific receptor. The transforming growth factor (TGF)‐β type I receptor (TβR‐I) inhibitor A‐83‐01 was expected to enhance the accumulation of nanocarriers...