Photodynamic therapy (PDT) functions when the light-excited photosensitizers transfer energy to oxygen molecules ( 3 O 2 ) to produce cytotoxic singlet oxygen ( 1 O 2 ) that can effectively kill cells or bacteria. However, the PDT efficacy is often reduced by the limited availability of 3 O 2 surrounding the photosensitizer and extremely short diffusion range of the photoactivated 1 O 2 . Herein, an enzymatic micromotor based on hollow mesoporous SiO 2 (mSiO 2 ) microspheres is constructed as a mobile and highly efficient photosensitizer platform. Carboxylated magnetic nanoparticles are connected with both hollow spheres and 5,10,15,20-tetrakis(4-aminophenyl)porphyrin molecules through covalent linkage between amino and carboxylic groups within a one-step reaction. Due to the intrinsic asymmetry of the mSiO 2 spheres, the micromotors can be propelled by ionic diffusiophoresis induced by the enzymatic decomposition of urea. Via numerical simulation, the self-propulsion mechanism is clarified and the movement direction is identified. By virtue of active self-propulsion, the current system can overcome the long-standing shortcomings of PDT and significantly enhance the PDT efficacy by improving the accessibility of the photosensitizer to 3 O 2 and enlarging the diffusing range of 1 O 2 . Therefore, by proposing a new solution to the bottleneck problems of PDT, this work provides insightful perspectives to the biomedical application of multifunctional micro/nanomotors. applications, including targeted drug delivery, mini-surgery, biochemical sensing, and diagnostics. [13][14][15] In particular, MNMs as active carriers with the capability of cargo loading and controllable motion have great potentials for effective delivery of different types of cargos. [15] So far, researchers have also explored stimuli-responsive materials, [16][17][18][19] biomimetic materials, [20][21][22] and micro-organisms functionalized with nanomaterials [23] as MNMs to precisely transport cargos of drugs, [16,20,23,24] proteins, [18,22,25] and genes [19] in vitro and/or in vivo. Compared with traditional passive delivery, MNMs can perform tasks such as controlled navigation, rapid transportation, and active delivery of payloads to disease sites, and thus have paved way for on demand biomedical cargo transportation. [15] Inspired by these achievements, we envision that self-propelled MNMs can serve as a mobile photosensitizer platform to improve the availability of 3 O 2 as well as the diffusion range of 1 O 2 , which can consequently achieve highly efficient PDT process.