期刊
PHARMACEUTICS
卷 15, 期 4, 页码 -出版社
MDPI
DOI: 10.3390/pharmaceutics15041284
关键词
PDT; antitumor efficacy; meso-arylporphyrins; erlotinib; conjugates; porphyrin metal complexes; Pluronic F127; polymer nanomicelles; nano-formulation
Photodynamic therapy (PDT) in oncology is a minimally invasive treatment option for cancer with minimal side effects and tissue scarring. This study focuses on the development and characterization of a new conjugate based on meso-arylporphyrin and a low-molecular-weight tyrosine kinase inhibitor, Erlotinib. A nano-formulation based on Pluronic F127 micelles was successfully prepared. The conjugate nanomicelles showed significantly enhanced activity and toxicity towards EGFR-overexpressing cancer cells compared to normal cells after irradiation.
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 mu M for the MDA-MB-231 cell line and 0.13 +/- 0.018 mu M for NKE cells after irradiation for the target conjugate nanomicelles.
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