Aug 2026· RSC Advances· Vol 16, pp. 47133 - 47137· 0 citations· 31 references
Medicine
TL;DR
Both in vitro and in vivo studies confirm that PFI effectively accumulates in tumors, relieves hypoxia, and achieves potent antitumor efficacy with negligible side effects, offering a facile and robust platform for hypoxia-tolerant photodynamic cancer therapy.
Abstract
Hypoxia-induced resistance remains a major obstacle in photodynamic therapy (PDT) due to the oxygen dependency of conventional type-II photosensitizers. To tackle this issue, we developed a phenothiazine-based small molecule (PFI) that integrates intrinsic oxygen-carrying perfluoroalkyl chains with type-I photodynamic functionality. The perfluorinated segments enable localized oxygen enrichment to counteract tumor hypoxia, while the phenothiazine core generates reactive oxygen species (ROS) via an oxygen-independent type-I pathway, sustaining phototoxicity even under low-oxygen environments. Both in vitro and in vivo studies confirm that PFI effectively accumulates in tumors, relieves hypoxia, and achieves potent antitumor efficacy with negligible side effects. This single-component design offers a facile and robust platform for hypoxia-tolerant photodynamic cancer therapy.
The intrinsic spatial heterogeneity of oxygen within solid tumors remains a formidable barrier to photodynamic therapy (PDT). Traditional Type II photosensitizers are incapacitated by hypoxia, while oxygen-independent Type I agents are generally hindered by a kinetic bottleneck in reactive oxygen species (ROS) producti...
This work provides an oxygen-unrestricted synergistic strategy to compensate for the limitations of standalone Type II PSs or HAPs monotherapy, offering valuable insights for clinical cancer treatment.
Porphyrin derivatives employed for photodynamic therapy (PDT) readily undergo intense π–π stacking, triggering drastic quenching of fluorescence and reactive oxygen species (ROS), which severely restricts their practical utilization in PDT research. In this work, meso-tetrakis(4-carboxyphenyl)porphyrin (TCPP) was ado...
Yuan-Jun Zhang, Guan-Huang Zhang, Yu-Feng Wang et al.· Inorganic Chemistry· 0 citations
Photodynamic therapy (PDT) is a light-activated modality that kills cells through photosensitizer-triggered reactive oxygen species, but its efficacy is strongly shaped by oxygen availability and by whether photochemistry proceeds through Type I or Type II pathways. In oxygen-rich settings, Type II PDT mainly generat...
I. V. da Cunha, M. Caetano, N. Bessas et al.· Biophysical Reviews· 0 citations
Porphyrin-based photosensitizers (PSs) are among the most widely explored agents for photodynamic therapy (PDT), yet their clinical translation is severely limited by poor biocompatibility, aggregation-induced quenching, insufficient tumor selectivity, and the intrinsic reactive oxygen species (ROS) resistance of cance...
Yi-Hui Ai, Chong-Zhi Wu, Zhi-Yao Li et al.· Small· 0 citations
Background Photodynamic therapy (PDT) eliminates malignancies through spatially controlled reactive oxygen species (ROS) generation and has achieved clinical success in localized tumors. Nevertheless, its therapeutic potential is severely restricted by the poor aqueous solubility, suboptimal ROS generation efficiency,...
Fang-Cheng Jiang, Yue Qin, Li Gao et al.· International Journal of Nan...· 0 citations
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