Engineering of BODIPY-based theranostics for cancer therapy

• BODIPY-based theranostics has good and tunable imaging and therapeutic modalities. • Molecular/nanoparticle engineering of BODIPY-based theranostics is elaborated. • Strategies to balance the imaging and therapy of the theranostics are summarized. • The review offers a guide to designing BODIPY-based theranostics in cancer therapy. In recent years, BODIPY-based theranostics have increasingly been used in cancer therapy and have achieved significant success. According to photochemical theories, the optical imaging ( e.g ., fluorescence [FLI]/photoacoustic [PAI]/photothermal imaging [PTI]) and phototherapy properties (photodynamic therapy [PDT] and photothermal therapy [PTT]) of BODIPY-based dyes can be well-tuned and balanced by chemical structural modifications. Furthermore, with the benefits of molecular/nanoparticle engineering, BODIPY-based theranostics can be endowed with versatile functionalities, including other cutting-edge therapeutic modalities, commendable tumor-targeting ability, and a delicate balance between imaging and therapy performance in a molecular/nano-entity, further enhancing its synergetic therapeutic potency and minimizing the undesirable side effects. In this review, we focus on BODIPY-based theranostics for tumor therapy and describe and discuss BODIPY-based FLI-guided chemotherapy, FLI-guided PDT, FLI-guided phototherapies, FLI-guided multi-modal therapies, and PAI-guided phototherapies, as well as multi-modal imaging-guided multi-modal therapies, particularly those that have become available in the last 3 years. The progress and bottlenecks of recent BODIPY-based theranostics are also itemized and discussed, describing the general design principles of BODIPY-based theranostics, with the aim of promoting the use of the theranostics in the clinical transformation of cancer therapy.