Carbon quantum dots (CDs) have attracted increased attention in recent decades because of their various applications in biosensing, bioimaging and drug delivery. In the present study, we have synthesized bifunctional ibuprofen-based carbon quantum dots (ICDs) using a simple one-step microwave-assisted method, for simultaneous bioimaging and anti-inflammatory effects. The ICDs exhibited high stability, low toxicity, negligible cytotoxicity and good biocompatibility in water. In particular, the produced ICDs demonstrated a decent imaging ability and excellent anti-inflammatory effects in vivo, making them potentially useful in bioimaging and future clinical treatment. Our results demonstrated that ICDs show promise in applications such as multifunctional biomaterials, depending on the selection of carbon sources, which would provide important guidance for the future design of multifunctional CDs in the field of biomedicine.