Labelled micelles for the delivery of cytotoxic Cu(II) and Ru(III) compounds in the treatment of aggressive orphan cancers: design and biological in vitro data
| Autor: | Stefano Merigliano, Dolores Fregona, Antonio Rosato, Patrizia Pontisso, Santina Quarta, Chiara Nardon, Nicolò Pettenuzzo, Pierfranco Conte, Isabella Monia Montagner, Leonardo Brustolin |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
Antineoplastic Agents
Poloxamer In Vitro Techniques 010402 general chemistry 01 natural sciences Biochemistry Micelle Inorganic Chemistry Microscopy Electron Transmission Cell Line Tumor Neoplasms Humans Dithiocarbamate Cytotoxicity Micelles chemistry.chemical_classification Drug Carriers 010405 organic chemistry Chemistry Spectrum Analysis Nuclear magnetic resonance spectroscopy Druglikeness Combinatorial chemistry In vitro 0104 chemical sciences Solubility Drug Design Drug delivery Ruthenium Compounds Nanocarriers Drug Screening Assays Antitumor Copper |
| Zdroj: | Università degli Studi di Padova-IRIS |
| Popis: | A recent study on our metal-dithiocarbamato complexes pointed out the antiproliferative properties and the druglikeness of some new patented derivatives. In this work, the best compounds have been encapsulated in micellar nanocarriers, being also carbohydrate-functionalized on their hydrophilic surface to investigate the possibility of a cancer-selective delivery. In particular, the nonionic block copolymer Pluronic® F127 (PF127) has been chemically modified with sugars and the derivatives characterized by means of NMR spectroscopy and FT-IR spectrophotometry. Then, the two selected complexes (β-[Ru2(PipeDTC)5]Cl (PipeDTC = piperidine dithiocarbamate) and [Cu(ProOMeDTC)2] (ProOMeDTC = L-proline methyl ester dithiocarbamate)), have been loaded into the hydrophobic core of PF127 micelles and cancer-targeting counterparts. These nanoformulations have been studied for their dimensions (DLS, TEM) and stability, and tested for their cytotoxicity against aggressive human cancer cell lines. The in vitro results were paralleled with mechanistic studies through Confocal Laser Scanning Microscopy and xCELLigence analysis. |
| Databáze: | OpenAIRE |
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