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.

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

Leonardo Brustolin
Investigation
;
Nicolò Pettenuzzo
Investigation
;
Chiara Nardon
Membro del Collaboration Group
;
Santina Quarta
Investigation
;
Isabella Montagner
Investigation
;
Patrizia Pontisso
Methodology
;
Antonio Rosato
Conceptualization
;
Pierfranco Conte
Funding Acquisition
;
Stefano Merigliano
Funding Acquisition
;
Dolores Fregona
Supervision
2020

Abstract

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.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11577/3352526
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