After the tremendous advances over the past two decades, micro‐/nanorobots can effectively convert other forms of energy into propulsion and movement, as well as be navigated to targeted locations under physiological conditions and environments. They have been demonstrated to have the potential to load, transport, and deliver therapeutic payloads directly to disease sites, thereby improving the therapeutic efficacy and reducing systemic side effects of highly toxic drugs. In this feature article, the various propulsion modalities of micro‐/nanorobots ranging from chemical/biochemical reactions to external fields, and to motile microorganisms are summarized and commented in terms of driving forces required by the automotive motion in biological media, biocompatibility, as well as the corresponding advantages and limitations in terms of biomedical applications. Then, the latest developments of in vitro and in vivo active drug delivery based on micro‐/nanorobots are discussed in detail. The challenges and future prospects are also highlighted in the end. With ever booming research enthusiasm in this field and increasing multidisciplinary cooperation, micro‐/nanorobots with intelligence and multifunctions will emerge in the near future, which would have a profound impact on the treatment of diseases.

Switchable chemotaxis is vital for motile microorganisms seeking benefits or to avoid harm. Inspired by nature, and for the first time, we demonstrate an artificial enzyme-powered micromotor that can autonomously regulate the propulsion mechanism, as well as motion directionality, by solely sensing the change of fuel concentration (Cf) in its surroundings. The as-designed micromotors have a pot-like microstructure with ureases immobilized on the inner surface. With the confined effect of the pot-like microstructure and unique features of the urease catalytic reaction, the molecular products are further reacted into ions, and their propulsion mechanism can be reversibly adjusted between ionic diffusiophoresis and microbubble recoils when Cf changes. Consequently, the as-developed micromotors under magnetic field are able to self-turn back if the local Cf differs greatly in their surroundings, indicating the achievement of positive and negative chemotaxis by sensing local Cf. Meanwhile, the micromotors also show highly enhanced migration speed by microbubble ejection, up to 60 μm/s, around 30 body lengths per second at physiological urea concentrations. Furthermore, they have an outer surface of mesoporous silica which is easily functionalized for applications such as stimuli-responsive delivery-associated therapies. This work will promote “smart” artificial micro/nanomotors for in vivo biomedical applications.