Polymeric micelle-mediated delivery of half-sandwich ruthenium(II) complexes with phosphanes derived from fluoroloquinolones for lung adenocarcinoma treatment.

Title Polymeric micelle-mediated delivery of half-sandwich ruthenium(II) complexes with phosphanes derived from fluoroloquinolones for lung adenocarcinoma treatment.
Authors P. Ko?oczek; A. Skórska-Stania; A. Cierniak; V. Sebastian; U.K. Komarnicka; M. P?otek; A. Kyzio?
Journal Eur J Pharm Biopharm
DOI 10.1016/j.ejpb.2018.04.016
Abstract

Novel half-sandwich ruthenium(II) complexes with aminomethyl(diphenyl)phosphine derived from fluoroloquinolones (RuPCp, RuPSf, RuPLm, RuPNr) were being investigated as alternatives to well-established metal-based chemotherapeutics. All compounds were characterized by elemental analysis, selected spectroscopic methods (i.e., absorption and fluorescence spectroscopies, ESI-MS, NMR, circular dichroizm), X-ray diffractometry, ICP-MS, and electrochemical techniques. To overcome low solubility, serious side effects connected with systemic cytotoxicity of ruthenium complexes, and acquiring the resistance of cancer cells, polymeric nanoformulations based on Pluronic P-123 micelles loaded with selected Ru(II) complexes were prepared and characterized. Resulting micelles (RuPCp_M, RuPNr_M) enabled efficient drug accumulation inside human lung adenocarcinoma (A549 tumor cell line), proved by confocal microscopy and ICP-MS analysis, allowing cytotoxic action. Studied complexes exhibited promising cytotoxicity in vitro with IC50 values significantly lower than the reference drug - cisplatin. The fluorescence spectroscopic data (CT-DNA titration, in vitro cell staining) together with analysis of DNA fragmentation (pBR322 plasmid, comet assay) provided clear evidence for the interaction with DNA inducing apoptotic cell death.

Citation P. Ko?oczek; A. Skórska-Stania; A. Cierniak; V. Sebastian; U.K. Komarnicka; M. P?otek; A. Kyzio?.Polymeric micelle-mediated delivery of half-sandwich ruthenium(II) complexes with phosphanes derived from fluoroloquinolones for lung adenocarcinoma treatment.. Eur J Pharm Biopharm. 2018;128:6981. doi:10.1016/j.ejpb.2018.04.016

Related Elements

Ruthenium

See more Ruthenium products. Ruthenium (atomic symbol: Ru, atomic number: 44) is a Block D, Group 8, Period 5 element with an atomic weight of 101.07. Ruthenium Bohr ModelThe number of electrons in each of ruthenium's shells is [2, 8, 18, 15, 1] and its electron configuration is [Kr] 4d7 5s1. The ruthenium atom has a radius of 134 pm and a Van der Waals radius of 207 pm. Ruthenium was discovered by Jędrzej Śniadecki in 1807. It was first recognized as a distinct element by Karl Ernst Claus in 1844. Elemental RutheniumIn its elemental form, ruthenium has a silvery white metallic appearance. Ruthenium is a rare transition metal belonging to the platinum group of metals. It is found in pentlandite, pyroxenite, and platinum group metal ores. The name Ruthenium originates from the Latin word "Ruthenia," meaning Russia.

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