LAUSR

Photodynamic therapy (PDT) is considered as an emerging therapeutic modality against cancer with high spatiotemporal selectivity because the utilized photosensitizers (PSs) are only active and toxic upon light irradiation. To maximize its effectiveness, PDT is usually applied repetitively for ablating various tumors. However, the total overdose of PSs from repeated administrations causes severe side effects. Herein, acidity‐activated graphene quantum dots‐based nanotransformers (GQD NT) are developed as PS vehicles for long‐period tumor imaging and repeated PDT. Under the guidance of Arg‐Gly‐Asp peptide, GQD NT targets to tumor tissues actively, and then loosens and enlarges in tumor acidity, thus promising long tumor retention. Afterwards, GQD NT transforms into small pieces for better penetration in tumor. Upon laser irradiation, GQD NT generates mild hyperthermia that enhances cell membrane permeability and further promotes the PSs uptake. Most intriguingly, the as‐prepared GQD NT not only “turns‐on” fluorescence/magnetic resonance signals, but also achieves efficient repeated PDT. Notably, the total PSs dose is reduced to 3.5 µmol kg−1, which is 10–30 times lower than that of other reported works. Overall, this study exploits a smart vehicle to enhance accumulation, retention, and release of PSs in tumors through programmed deformation, thus overcoming the overdose obstacle in repeated PDT.