Borisenkova Alina A, Baykov Dmitriy V, Titova Anna V, Bakhmetyev Vadim V, Markova Maria A, Lyutova Zhanna B, Popugaev Anton V, Khaleev Vladislav S, Sedov Victor P
Radiation Technology Department, St. Petersburg State Institute of Technology (Technical University), 190013 St. Petersburg, Russia.
Petersburg Nuclear Physics Institute named by B.P. Konstantinov of National Research Centre "Kurchatov Institute", 188300 Gatchina, Russia.
Molecules. 2025 Jun 24;30(13):2718. doi: 10.3390/molecules30132718.
Folic acid (FA) is used as a targeting ligand for targeted drug delivery to tumor cells, some types of which overexpress folate receptors on their surface. However, while the preparation of conjugates containing FA may comprise a multi-step process, FA presents low photostability under UV irradiation. In addition, FA undergoes radiolysis under the action of ionizing radiation, which is utilized for drug sterilization. In this study, we investigate the stability of FA in a conjugate (FA-PVP-C) with fullerene C and polyvinylpyrrolidone under the action of UV (205-400 nm) and electron irradiation (doses from 2 to 8 kGy) at different pH (4.5, 7.2, 10.7). The degradation of FA is studied using fluorescence and UV-Vis spectroscopy. It is found that the fullerene C in the FA-PVP-C conjugate suppresses the degradation of FA during both photolysis and radiolysis, which is confirmed by the decrease in the quantum yield of fluorescence and the radiation chemical yield of FA destruction accompanied by increasing fullerene content in the conjugate (from 2.8 to 10 wt.%).
叶酸（FA）被用作靶向配体，用于将药物靶向递送至肿瘤细胞，其中一些肿瘤细胞表面过度表达叶酸受体。然而，虽然制备含FA的缀合物可能包括多步过程，但FA在紫外线照射下光稳定性较低。此外，FA在用于药物灭菌的电离辐射作用下会发生辐射分解。在本研究中，我们研究了在不同pH值（4.5、7.2、10.7）下，FA与富勒烯C和聚乙烯吡咯烷酮形成的缀合物（FA-PVP-C）在紫外线（205 - 400 nm）和电子辐照（剂量为2至8 kGy）作用下的稳定性。使用荧光光谱和紫外可见光谱研究了FA的降解情况。结果发现，FA-PVP-C缀合物中的富勒烯C在光解和辐射分解过程中均抑制了FA的降解，这通过荧光量子产率的降低以及FA破坏的辐射化学产率的降低得到证实，同时缀合物中富勒烯含量增加（从2.8 wt.%至10 wt.%）。
