Toxicological research of novel nanomaterials is a major developmental step of their clinical approval. Since iron oxide magnetic nanoparticles have a great potential in cancer treatment and diagnostics, the investigation of their toxic properties is very topical. In this paper we synthesized bovine serum albumin‐coated iron oxide nanoparticles with different sizes and their polyethylene glycol derivative. To prove high biocompatibility of obtained nanoparticles the number of in vitro toxicological tests on human fibroblasts and U251 glioblastoma cells was performed. It was shown that albumin nanoparticles’ coating provides a stable and biocompatible shell and prevents cytotoxicity of magnetite core. On long exposure times (48 hours), cytotoxicity of iron oxide nanoparticles takes place due to free radical production, but this toxic effect may be neutralized by using polyethylene glycol modification.
We
report herein the design, synthesis, and biological investigation
of a series of novel Pt(IV) prodrugs with non-steroidal anti-inflammatory
drugs naproxen, diclofenac, and flurbiprofen, as well as these with
stearic acid in the axial position. Six Pt(IV) prodrugs 5–10 were designed, which showed superior antiproliferative activity
compared to cisplatin as well as an ability to overcome tumor cell
line resistance to cisplatin. By tuning the drug lipophilicity via
variation of the axial ligands, the most potent Pt(IV) prodrug 7 was obtained, with an enhanced cellular accumulation of
up to 153-fold that of cisplatin and nanomolar cytotoxicity both in
2D and 3D cell cultures. Pt2+ species were detected at
different depths of MCF-7 spheroids after incubation with Pt(IV) prodrugs
using a Pt-coated carbon nanoelectrode. Cisplatin accumulation in
vivo in the murine mammary EMT6 tumor tissue of BALB/c mice after
Pt(IV) prodrug injection was proved electrochemically as well. The
drug tolerance study on BALB/c mice showed good tolerance of 7 in doses up to 8 mg/kg.
Recently, a new class of prokaryotic compartments, collectively called encapsulins or protein nanocompartments, has been discovered. The shell proteins of these structures self-organize to form icosahedral compartments with a diameter of 25–42 nm, while one or more cargo proteins with various functions can be encapsulated in the nanocompartment. Non-native cargo proteins can be loaded into nanocompartments and the surface of the shells can be further functionalized, which allows for developing targeted drug delivery systems or using encapsulins as contrast agents for magnetic resonance imaging. Since the genes encoding encapsulins can be integrated into the cell genome, encapsulins are attractive for investigation in various scientific fields, including biomedicine and nanotechnology.
A series
of 73 ligands and 73 of their Cu+2 and Cu+1 copper
complexes with different geometries, oxidation states
of the metal, and redox activities were synthesized and characterized.
The aim of the study was to establish the structure–activity
relationship within a series of analogues with different substituents
at the N(3) position, which govern the redox potentials of the Cu+2/Cu+1 redox couples, ROS generation ability, and
intracellular accumulation. Possible cytotoxicity mechanisms, such
as DNA damage, DNA intercalation, telomerase inhibition, and apoptosis
induction, have been investigated. ROS formation in MCF-7 cells and
three-dimensional (3D) spheroids was proven using the Pt-nanoelectrode.
Drug accumulation and ROS formation at 40–60 μm spheroid
depths were found to be the key factors for the drug efficacy in the
3D tumor model, governed by the Cu+2/Cu+1 redox
potential. A nontoxic in vivo single-dose evaluation
for two binuclear mixed-valence Cu+1/Cu+2 redox-active
coordination compounds, 72k and 61k, was
conducted.
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