Application Of BODIPY-based Nanomaterials In Bioimaging And Cancer Therapy

Cancer is increasingly threatening human health.Traditional treatments such as surgery,radiotherapy and chemotherapy have the disadvantages of large trauma,weak selectivity and strong side effects.Therefore,it is urgent to develop new tumor treatment options.Borondipyrromethane fluorescent dye(BODIPY)has become the focus of attention in recent years due to its good photophysical and photochemical properties and outstanding performance in the field of biomedical nanomaterials.However,the poor solubility of BODIPY in water greatly limits its application in the field of tumor treatment.In this paper,we synthesized BODIPY-based nanomaterials with different physicochemical properties and realized their applications in bioimaging and tumor therapy.The specific work is as follows:1.Near-Infrared BODIPY J-aggregates for photothermal therapyWe have synthesized the BODIPY derivative BDP-(NO₂)₃ containing three nitro groups,which exhibits a J-aggregates characteristic with significant absorption red-shift in organic solvents and water.BDP-(NO₂)₃ nanoparticles(NPs)could be prepared by supramolecular co-assembly from BDP-(NO₂)₃ and poly(oxyethylene)-poly(oxypropylene)copolymer(poloxamer F-127).BDP-(NO₂)₃ NPs still exhibit a significant J-aggregates characteristic,and have the advantages of good water dispersibility,excellent biosafety,high photothermal conversion efficiency,near-infrared(NIR)absorption,thus being applicable to photothermal therapy of tumors.In vitro and in vivo experiments demonstrated that BDP-(NO₂)₃ NPs could effectively inhibit the proliferation of cancer cells and lead to tumor ablation.2.Application of PTX-S-BDP nano-prodrug in imaging and treatment of tumor cellsThe development of controlled release prodrugs with high drug loading can greatly improve the efficacy of chemotherapy.We prepared a tumor microenvironment-responsive prodrug,PTX-S-BDP,using redox-responsive groups bridging paclitaxel(PTX)and BODIPY(BDP-OH)for fluorescence imaging-guided chemotherapy.PTX-S-BDP NPs were obtained by co-assembly of PTX-S-BDP with F-127.Real-time cellular localization of chemotherapeutic agents via BDP-OH fluorescence was facilitated by visualization of chemotherapy.In vitro experiments showed that PTX-S-BDP NPs exhibited cytotoxicity comparable to paclitaxel,excellent cellular imaging,and better cell selectivity to cancer cells.This novel nano-prodrug overcomes the problems of small molecule drugs such as hydrophobicity,low drug loading,drug retention and premature release,and provides a certain reference value for the development of nano-prodrugs in the future.