(AGENPARL) – LONDON (UNITED KINGDOM), mer 30 settembre 2020
Organic nanomaterials with efficient ROS generation and high photothermal conversion efficiency have emerged as a new generation of therapeutic agents for PDT/PTT synergistic cancer treatment. However, most of the organic nanomaterials exhibited weak emission in water because of the aggregation-caused quenching (ACQ) effect, which seriously hampers their biological applications in fluorescence bioimaging. In this study, we design and synthesize a new organic small molecule (T-BDP) with donor-acceptor-donor (D-A-D) structure by conjugation of boron-dipyrromethene (BODIPY) and triphenylamine (TPA). Moreover, a 1,8-naphthalenediimide (NI) structure with electron-withdrawing ability is introduced onto the core of BODIPY to further enhance the intramolecular charge transfer, leading to the redshift of absorption to the near-infrared region. T-BDP displays the significant aggregation-induced emission (AIE) performance, probably due to the presence of two twisted TPA groups onto BODIPY core. Accordingly, after self-assembly into nanoparticles, T-BDP NPs exhibits strong near-infrared emission in the water. Under a single 635 nm laser irradiation, T-BDP NPs could generate reactive oxygen species and heat simultaneously. The photothermal conversion efficiency of T-BDP NPs is determined to be 50.9%. The low dark toxicity and high photocytoxicity of T-BDP NPs are verified against A549 cells by MTT assay and AM/PI staining method. Due to the strong emission of T-BDP NPs, their accumulation and subcellular localization in cancer cells are observed by a laser confocal fluorescence microscope. The results demonstrate that T-BDP NPs are mainly located in lysosomes of cancer cells. Thus, the as-prepared small molecule-based AIE nanoparticles holds great potential for fluorescence imaging-guided PDT/PTT synergistic tumor therapy.
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