Research output: Contribution to journal › Article › peer-review
Synthesis and Biological Properties of EGFR-Targeted Photosensitizer Based on Cationic Porphyrin. / Bortnevskaya, Yulia S.; Shiryaev, Nikita A.; Zakharov, Nikita S.; Kitoroage, Oleg O.; Gradova, Margarita A.; Karpechenko, Natalia Yu.; Novikov, Alexander S.; Nikolskaya, Elena D.; Mollaeva, Mariia R.; Yabbarov, Nikita G.; Bragina, Natal’ya A.; Zhdanova, Kseniya A.
In: Pharmaceutics, Vol. 15, No. 4, 1284, 19.04.2023.Research output: Contribution to journal › Article › peer-review
}
TY - JOUR
T1 - Synthesis and Biological Properties of EGFR-Targeted Photosensitizer Based on Cationic Porphyrin
AU - Bortnevskaya, Yulia S.
AU - Shiryaev, Nikita A.
AU - Zakharov, Nikita S.
AU - Kitoroage, Oleg O.
AU - Gradova, Margarita A.
AU - Karpechenko, Natalia Yu.
AU - Novikov, Alexander S.
AU - Nikolskaya, Elena D.
AU - Mollaeva, Mariia R.
AU - Yabbarov, Nikita G.
AU - Bragina, Natal’ya A.
AU - Zhdanova, Kseniya A.
PY - 2023/4/19
Y1 - 2023/4/19
N2 - Photodynamic therapy (PDT) in oncology is characterized by low invasiveness, minimal side effects, and little tissue scarring. Increasing the selectivity of PDT agents toward a cellular target is a new approach intended to improve this method. This study is devoted to the design and synthesis of a new conjugate based on meso-arylporphyrin with a low-molecular-weight tyrosine kinase inhibitor, Erlotinib. A nano-formulation based on Pluronic F127 micelles was obtained and characterized. The photophysical and photochemical properties and biological activity of the studied compounds and their nano-formulation were studied. A significant, 20-40-fold difference between the dark and photoinduced activity was achieved for the conjugate nanomicelles. After irradiation, the studied conjugate nanomicelles were 1.8 times more toxic toward the EGFR-overexpressing cell line MDA-MB-231 compared to the conditionally normal NKE cells. The IC50 was 0.073 ± 0.014 μM for the MDA-MB-231 cell line and 0.13 ± 0.018 μM for NKE cells after irradiation for the target conjugate nanomicelles.
AB - Photodynamic therapy (PDT) in oncology is characterized by low invasiveness, minimal side effects, and little tissue scarring. Increasing the selectivity of PDT agents toward a cellular target is a new approach intended to improve this method. This study is devoted to the design and synthesis of a new conjugate based on meso-arylporphyrin with a low-molecular-weight tyrosine kinase inhibitor, Erlotinib. A nano-formulation based on Pluronic F127 micelles was obtained and characterized. The photophysical and photochemical properties and biological activity of the studied compounds and their nano-formulation were studied. A significant, 20-40-fold difference between the dark and photoinduced activity was achieved for the conjugate nanomicelles. After irradiation, the studied conjugate nanomicelles were 1.8 times more toxic toward the EGFR-overexpressing cell line MDA-MB-231 compared to the conditionally normal NKE cells. The IC50 was 0.073 ± 0.014 μM for the MDA-MB-231 cell line and 0.13 ± 0.018 μM for NKE cells after irradiation for the target conjugate nanomicelles.
KW - PDT
KW - Pluronic F127
KW - antitumor efficacy
KW - conjugates
KW - erlotinib
KW - meso-arylporphyrins
KW - nano-formulation
KW - polymer nanomicelles
KW - porphyrin metal complexes
UR - https://www.mendeley.com/catalogue/668279f3-3885-34ec-85b1-703ff144c21d/
U2 - 10.3390/pharmaceutics15041284
DO - 10.3390/pharmaceutics15041284
M3 - Article
C2 - 37111769
VL - 15
JO - Pharmaceutics
JF - Pharmaceutics
SN - 1999-4923
IS - 4
M1 - 1284
ER -
ID: 104537765