The aim of the present study was the proposal of a strategy to permit the safe use of the powerful antitumor agent Cisplatin. Considering the possibility of reducing the oxidative stress responsible for the Cisplatin induced nephrotoxicity by using antioxidants, such as flavonoids, we proposed the concomitant therapeutic association of Cisplatin with Quercetin. Considering the poor solubility of Quercetin, nanoemulsions have been proposed to encapsulate and facilitate the use of the drug. Originally, the concomitant encapsulation of Quercetin with Cisplatin has been also assessed. The obtained formulations have been characterized and tested against two human cell models, namely the human breast cancer MDA-MB-231 and the normal HEK-293 renal cells. We demonstrated that the new formulated nanoemulsions have improved the anticancer properties of both the molecules and, most importantly, the synergistic effect of the Cisplatin/Quercetin against the MDA-MB-231. Moreover, the dramatic cytotoxic effects of Cisplatin against the human renal HEK-293 cells have been significantly diminished by the use of nanoemulsions containing both the molecules, whereas the antioxidant properties of encapsulated Quercetin have been improved. Finally, the simple process used to obtain the nanoemulsions and the physico-chemical properties compatible with parenteral administration, the stability and the improved pharmaceutical effects contribute to the high potential of this strategy to be studied in future in vivo studies.

A winning strategy to improve the anticancer properties of Cisplatin and Quercetin based on the nanoemulsions formulation

Ceramella J.;Mariconda A.;Saturnino C.;Longo P.;
2021

Abstract

The aim of the present study was the proposal of a strategy to permit the safe use of the powerful antitumor agent Cisplatin. Considering the possibility of reducing the oxidative stress responsible for the Cisplatin induced nephrotoxicity by using antioxidants, such as flavonoids, we proposed the concomitant therapeutic association of Cisplatin with Quercetin. Considering the poor solubility of Quercetin, nanoemulsions have been proposed to encapsulate and facilitate the use of the drug. Originally, the concomitant encapsulation of Quercetin with Cisplatin has been also assessed. The obtained formulations have been characterized and tested against two human cell models, namely the human breast cancer MDA-MB-231 and the normal HEK-293 renal cells. We demonstrated that the new formulated nanoemulsions have improved the anticancer properties of both the molecules and, most importantly, the synergistic effect of the Cisplatin/Quercetin against the MDA-MB-231. Moreover, the dramatic cytotoxic effects of Cisplatin against the human renal HEK-293 cells have been significantly diminished by the use of nanoemulsions containing both the molecules, whereas the antioxidant properties of encapsulated Quercetin have been improved. Finally, the simple process used to obtain the nanoemulsions and the physico-chemical properties compatible with parenteral administration, the stability and the improved pharmaceutical effects contribute to the high potential of this strategy to be studied in future in vivo studies.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11386/4773028
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