1. Fullerene C 60 Conjugate with Folic Acid and Polyvinylpyrrolidone for Targeted Delivery to Tumor Cells.
- Author
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Borisenkova AA, Bolshakova OI, Titova AV, Ryabokon IS, Markova MA, Lyutova ZB, Sedov VP, Varfolomeeva EY, Bakhmetyev VV, Arutyunyan AV, Burdakov VS, and Sarantseva SV
- Subjects
- Humans, Cell Line, Tumor, A549 Cells, HeLa Cells, Particle Size, Folic Acid chemistry, Folic Acid pharmacology, Povidone chemistry, Fullerenes chemistry, Fullerenes pharmacology, Drug Delivery Systems methods
- Abstract
The use of targeted drug delivery systems, including those based on selective absorption by certain receptors on the surface of the target cell, can lead to a decrease in the minimum effective dose and the accompanying toxicity of the drug, as well as an increase in therapeutic efficacy. A fullerene C
60 conjugate (FA-PVP-C60 ) with polyvinylpyrrolidone (PVP) as a biocompatible spacer and folic acid (FA) as a targeting ligand for tumor cells with increased expression of folate receptors (FR) was obtained. Using13 C NMR spectroscopy, FT-IR, UV-Vis spectrometry, fluorometry and thermal analysis, the formation of the conjugate was confirmed and the nature of the binding of its components was established. The average particle sizes of the conjugate in aqueous solutions and cell culture medium were determined using dynamic light scattering (DLS) and nanoparticle tracking analysis (NTA). The FA-PVP-C60 showed antiradical activity against• DPPH,• OH and O2 • - , but at the same time, it was shown to generate1 O2 . It was found that the conjugate in the studied concentration range (up to 200 μg/mL) is non-toxic in vitro and does not affect the cell cycle. To confirm the ability of the conjugate to selectively accumulate through folate-mediated endocytosis, its uptake into cells was analyzed by flow cytometry and confocal microscopy. It was shown that the conjugate is less absorbed by A549 cells with low FR expression than by HeLa, which has a high level of expression of this receptor.- Published
- 2024
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