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With targeting and entering into bioorthogonal molecule azide‐prelabeled tumor cells, the nanoparticles release EA under the acidic and high GSH environment to inhibit GST activity, while released nitric oxide (NO) from donor GSNO triggered by GSH improves cisplatin uptake, both processes pronouncedly deplete GSH due to simultaneous GSH consumption, collectively reversing cisplatin resistance and inhibiting the growth of cisplatin‐resistant orthotopic non‐small cell lung cancer after nebulization