Near-Infrared Triggered Upconversion Polymeric Nanoparticles Based on Aggregation-Induced Emission and Mitochondria Targeting for Photodynamic Cancer Therapy

ACS Appl Mater Interfaces. 2017 Aug 16;9(32):26731-26739. doi: 10.1021/acsami.7b07768. Epub 2017 Aug 2.


Photodynamic therapy (PDT) is an auspicious strategy for cancer therapy by yielding reactive oxygen species (ROS) under light irradiation. Here, we have developed near-infrared (NIR) triggered polymer encapsulated upconversion nanoparticles (UCNPs) based on aggregation-induced emission (AIE) characteristics and mitochondria target ability for PDT. The coated AIE polymer as a photosensitizer can be photoactivated by the up-converted energy of UCNPs upon 980 nm laser irradiation, which could generate ROS efficiently in mitochondria and induce cell apoptosis. Moreover, a "sheddable" poly(ethylene glycol) (PEG) layer was easily conjugated at the surface of NPs. The pH-responsive PEG layer shields the surface positive charges and shows stronger protein-resistance ability. In the acidic tumor environment, PEGylated NPs lose the PEG layer and show the mitochondria-targeting ability by responding to tumor acidity. A cytotoxicity study indicated that these NPs have good biocompatibility in the dark but exert severe cytotoxicity to cancer cells, with only 10% cell viability, upon being irradiated with an NIR laser. The AIE nanoparticles are a good candidate for effective mitochondria targeting photosensitizer for PDT.

Keywords: aggregation-induced emission; cancer cells; mitochondria; photodynamic therapy; upconversion nanoparticles.

MeSH terms

  • Humans
  • Mitochondria
  • Nanoparticles*
  • Neoplasms
  • Photochemotherapy
  • Photosensitizing Agents


  • Photosensitizing Agents