TY - JOUR
T1 - Photochemical Internalization with Fimaporfin: Enhanced Bleomycin Treatment for Head and Neck Cancer
AU - Enzian, Paula
AU - Rahmanzadeh, Ramtin
N1 - @Article{pharmaceutics15082040,
AUTHOR = {Enzian, Paula and Rahmanzadeh, Ramtin},
TITLE = {Photochemical Internalization with Fimaporfin: Enhanced Bleomycin Treatment for Head and Neck Cancer},
JOURNAL = {Pharmaceutics},
VOLUME = {15},
YEAR = {2023},
NUMBER = {8},
ARTICLE-NUMBER = {2040},
URL = {https://www.mdpi.com/1999-4923/15/8/2040},
ISSN = {1999-4923},
ABSTRACT = {Head and neck squamous cell carcinoma (HNSCC) still represents the world’s sixth most common tumor entity, with increasing incidence. The reachability of light makes HNSCC suitable for light-based therapies such as Photochemical Internalization (PCI). The drug Bleomycin is cytotoxic and used as an anti-tumor medication. Since Bleomycin is endocytosed as a relatively large molecule, part of it is degraded in lysosomes before reaching its intracellular target. The goal of our study was to improve the intracellular availability of Bleomycin with PCI. We investigate the intracellular delivery of Bleomycin after PCI with the photosensitizer Fimaporfin. A systematic variation of Bleomycin and Fimaporfin concentrations and light irradiation led to the pronounced cell death of HNSCC cells. After optimization, the same level of tumor cell death of 75% was reached with a 20-fold lower Bleomycin concentration. This would allow treatment of HNSCC with high local tumor cell death and reduce the side effects of Bleomycin, e.g., lung fibrosis, at the same time. This demonstrates the increased efficacy of the anti-tumor medication Bleomycin in combination with PCI.},
DOI = {10.3390/pharmaceutics15082040}
}
Publisher Copyright:
© 2023 by the authors.
PY - 2023/7/28
Y1 - 2023/7/28
N2 - Head and neck squamous cell carcinoma (HNSCC) still represents the world’s sixth most common tumor entity, with increasing incidence. The reachability of light makes HNSCC suitable for light-based therapies such as Photochemical Internalization (PCI). The drug Bleomycin is cytotoxic and used as an anti-tumor medication. Since Bleomycin is endocytosed as a relatively large molecule, part of it is degraded in lysosomes before reaching its intracellular target. The goal of our study was to improve the intracellular availability of Bleomycin with PCI. We investigate the intracellular delivery of Bleomycin after PCI with the photosensitizer Fimaporfin. A systematic variation of Bleomycin and Fimaporfin concentrations and light irradiation led to the pronounced cell death of HNSCC cells. After optimization, the same level of tumor cell death of 75% was reached with a 20-fold lower Bleomycin concentration. This would allow treatment of HNSCC with high local tumor cell death and reduce the side effects of Bleomycin, e.g., lung fibrosis, at the same time. This demonstrates the increased efficacy of the anti-tumor medication Bleomycin in combination with PCI.
AB - Head and neck squamous cell carcinoma (HNSCC) still represents the world’s sixth most common tumor entity, with increasing incidence. The reachability of light makes HNSCC suitable for light-based therapies such as Photochemical Internalization (PCI). The drug Bleomycin is cytotoxic and used as an anti-tumor medication. Since Bleomycin is endocytosed as a relatively large molecule, part of it is degraded in lysosomes before reaching its intracellular target. The goal of our study was to improve the intracellular availability of Bleomycin with PCI. We investigate the intracellular delivery of Bleomycin after PCI with the photosensitizer Fimaporfin. A systematic variation of Bleomycin and Fimaporfin concentrations and light irradiation led to the pronounced cell death of HNSCC cells. After optimization, the same level of tumor cell death of 75% was reached with a 20-fold lower Bleomycin concentration. This would allow treatment of HNSCC with high local tumor cell death and reduce the side effects of Bleomycin, e.g., lung fibrosis, at the same time. This demonstrates the increased efficacy of the anti-tumor medication Bleomycin in combination with PCI.
UR - http://www.scopus.com/inward/record.url?scp=85168906630&partnerID=8YFLogxK
UR - https://www.mendeley.com/catalogue/e8a449a9-1145-3402-bbcf-63f89349eb0f/
U2 - 10.3390/pharmaceutics15082040
DO - 10.3390/pharmaceutics15082040
M3 - Journal articles
C2 - 37631254
SN - 1999-4923
VL - 15
JO - Pharmaceutics
JF - Pharmaceutics
IS - 8
M1 - 2040
ER -
