Acs Applied Materials & Interfaces: Tumor activated water-soluble photosensitizers for near-infrared photodynamic cancer therapy
作者：Hu Xiong, Kejin Zhou, Yunfeng Yan, Jason B. Miller, and Daniel J. Siegwart
關鍵字：photodynamic therapy, photosensitizer, activatable nanoprobes, near-infrared, pH-responsive fluorescence imaging
論文來源：期刊
具體來源：Acs Applied Materials & Interfaces
發表時間：2018年
Current photosensitizers (PSs) for photodynamic therapy (PDT) are limited by their low water
solubility and tendency to aggregate, low near-infrared (NIR)
absorption, and low cancer selectivity. Here, we designed
iodinated, water-soluble NIR boron dipyrromethene-based PSs
to achieve image-guided and efficient PDT against cancer in
vivo that is enhanced by leveraging tumor-specific pHresponsive activation. PEG2k5c-I and PEG2k5c-OMe-I
localized to tumors and were activated by acidic pH in the
tumor microenvironment to produce 1O2 and fluorescence for
efficient PDT and effective cancer detection after intravenous administration. Upon NIR irradiation, these PSs exhibited strong
NIR absorption at 660 and 690 nm, stable NIR emission at 692 and 742 nm, and high 1O2 quantum yields of 0.78 and 0.72 in
acidic pH. PEG2k5c-I and PEG2k5c-OMe-I killed cancer cells upon irradiation of NIR light and were nontoxic without
irradiation. Light-activated PDT treatment of breast cancer tumors in mice resulted in suppression of tumor growth, DNA
damage, and necrosis selectively in tumors. This work thus introduces a versatile method to directly synthesize modular pHresponsive water-soluble PSs and provides a versatile strategy for activatable PDT against cancer.