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Targeted drug delivery based on polymeric nanoparticles has been a long‐standing interest in nanomedicine for its beneficial traits including controlled and localized drug release. Gas‐responsive polymers offer an advantageous platform and have been slowly gaining attention in spatially locating and displaying unique interactions of specific responsive chemical entities in polymeric chains with endogenous gaseous stimuli. In this review, we highlight recent developments in polymeric nanoformulations with stimulant chemical entities for gasotransmittors such as NO, CO, H2S, SO2, O2 and CO2 in enhancing efficacy in therapeutic interventions. We underline some challenges and limitations of exploring these systems for clinical applications, and how we can further tap into the potential of these emerging materials. © 2021 Society of Industrial Chemistry. [ABSTRACT FROM AUTHOR]