<p>The development of tumor-targeted multimodality therapy is an important strategy to improve the curative effects of cancer treatment. It is critical to construct such a platform that can perfectly integrate these functional entities into one. Herein, we designed a phenyl sulfonamide-modified pillararene WP5-PEG-BSA. WP5-PEG-BSA can be used to construct endoplasmic reticulum (ER)-targeting nanocarriers. Then NO donor <i>S</i>-nitroso-<i>N</i>-acetyl-<i>D</i>-penicillamine (SNAP) and the newly designed photosensitizer DPP-DMATPE were loaded into the nanocarriers via different paths. Under laser irradiation, DPP-DMATPE exhibited excellent type I photodynamic activity, while SNAP can release NO under the action of glutathione. The formed nanodrugs BSA-DPP/SNAP exhibited outstanding ER-targeting and high lethality towards tumor cells as well as biocompability. What’s even more worth saying is that BSA-DPP/SNAP performed well even in hypoxic tumor cells. The final experimental results <i>in vivo</i> again confirmed the good therapeutic effects of BSA-DPP/SNAP. As a result, a supramolecular nanoplatform that realizes highly efficient ER-targeting type I photodynamic and NO gas cancer therapy was constructed.</p>

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Pillararene based supramolecular nanoplatform for endoplasmic reticulum-targeting type I photodynamic and NO gas therapy

  • Shaoqi Xie,
  • Chang Liu,
  • Yue Cao,
  • Jiachen Xia,
  • Bing Lu

摘要

The development of tumor-targeted multimodality therapy is an important strategy to improve the curative effects of cancer treatment. It is critical to construct such a platform that can perfectly integrate these functional entities into one. Herein, we designed a phenyl sulfonamide-modified pillararene WP5-PEG-BSA. WP5-PEG-BSA can be used to construct endoplasmic reticulum (ER)-targeting nanocarriers. Then NO donor S-nitroso-N-acetyl-D-penicillamine (SNAP) and the newly designed photosensitizer DPP-DMATPE were loaded into the nanocarriers via different paths. Under laser irradiation, DPP-DMATPE exhibited excellent type I photodynamic activity, while SNAP can release NO under the action of glutathione. The formed nanodrugs BSA-DPP/SNAP exhibited outstanding ER-targeting and high lethality towards tumor cells as well as biocompability. What’s even more worth saying is that BSA-DPP/SNAP performed well even in hypoxic tumor cells. The final experimental results in vivo again confirmed the good therapeutic effects of BSA-DPP/SNAP. As a result, a supramolecular nanoplatform that realizes highly efficient ER-targeting type I photodynamic and NO gas cancer therapy was constructed.