Key Laboratory for Organic Electronics and Information Displays and Institute of Advanced Materials, Nanjing University of Posts and Telecommunications, Nanjing 210023, Jiangsu, P.R. China.
Biomater Sci. 2021 Mar 21;9(6):2115-2123. doi: 10.1039/d0bm01863e. Epub 2021 Jan 22.
The simultaneous near-infrared (NIR)-absorbed photodynamic therapy (PDT)/photothermal therapy (PTT) has proved to be a promising approach to increase the antitumor efficiency due to their synergistic effect. Herein, a boron dipyrromethene (BODIPY)-based photosensitizer was designed and synthesized for the enhanced synergistic NIR-absorbed PDT/PTT therapy upon NIR light irradiation. In this strategy, a three-dimensional rigid polyhedral oligomeric silsesquioxane (POSS) block was introduced into the Br-BODIPY molecule to alleviate the aggregation of the photosensitizer. The POSS hybrid BODIPY (Br-BODIPY-POSS) was further functionalized with a biocompatible amphiphilic PEG via a facile thiol-ene "click" reaction, affording Br-BODIPY-POSS-PEG (BBPP). BBPP can self-assemble into nanoparticles, which maintain a competitive photothermal conversion efficiency (η = 30.2%) with its counterpart Br-BODIPY-PEG (BBP, η = 34.5%). Significantly, BBPP exhibited a relatively higher oxygen quantum yield (Φ = 0.405) than BBP (Φ = 0.175). The in vitro and in vivo experiments showed that BBPP possessed negligible dark cytotoxicity and a better phototherapeutic outcome than BBP. The proof-of-concept of the POSS hybrid photosensitizer offers guidance for the construction of single-component and PDT/PTT-balanced NIR nanoagents to promote the cancer therapeutic efficacy in the future.
同时近红外（NIR）吸收的光动力疗法（PDT）/光热疗法（PTT）已被证明是一种很有前途的方法，可以提高抗肿瘤效率，因为它们具有协同作用。在此，设计并合成了一种基于硼二吡咯甲川（BODIPY）的光敏剂，用于在近红外光照射下增强协同 NIR 吸收 PDT/PTT 治疗。在该策略中，将三维刚性聚倍半硅氧烷（POSS）块引入 Br-BODIPY 分子中，以减轻光敏剂的聚集。通过简单的硫醇-烯“点击”反应，将 POSS 杂化 BODIPY（Br-BODIPY-POSS）进一步功能化，得到 Br-BODIPY-POSS-PEG（BBPP）。BBPP 可以自组装成纳米颗粒，其光热转换效率（η = 30.2%）与 Br-BODIPY-PEG（BBP，η = 34.5%）相当。值得注意的是，BBPP 的氧量子产率（Φ = 0.405）高于 BBP（Φ = 0.175）。体外和体内实验表明，BBPP 具有可忽略的暗毒性和比 BBP 更好的光治疗效果。POSS 杂化光敏剂的概念验证为构建单一成分和 PDT/PTT 平衡的 NIR 纳米制剂提供了指导，以提高未来癌症的治疗效果。
