We report here the preparation, physico-chemical characterization, and biological evaluation of a new liposome formulation as a tool for tumor angiogenesis inhibition. Liposomes are loaded with sunitinib, a tyrosine kinase inhibitor, and decorated with cyclo-aminoprolineRGD units (cAmpRGD), efficient and selective ligands for integrin α V β 3 . The RGD units play multiple roles since they target the nanovehicles at the integrin α V β 3 -overexpressing cells (e.g. activated endothelial cells), favor their active cell internalization, providing drug accumulation in the cytoplasm, and likely take part in the angiogenesis inhibition by interfering in the α V β 3 -VEGFR2 cross-talk. Both in vitro and in vivo studies show a better efficacy of this integrated antiangiogenic tool with respect to the free sunitinib and untargeted sunitinib-loaded liposomes. This system could allow a lower administration of the drug and, by increasing the vector specificity, reduce side-effects in a prolonged antiangiogenic therapy.

Integrin-targeted AmpRGD sunitinib liposomes as integrated antiangiogenic tools / Bianchini, Francesca; De Santis, Augusta; Portioli, Elisabetta; Russo Krauss, Irene; Battistini, Lucia; Curti, Claudio; Peppicelli, Silvia; Calorini, Lido; D'Errico, Gerardino; Zanardi, Franca; Sartori, Andrea. - In: NANOMEDICINE. - ISSN 1549-9634. - 18:(2019), pp. 135-145. [10.1016/j.nano.2019.02.015]

Integrin-targeted AmpRGD sunitinib liposomes as integrated antiangiogenic tools

Portioli, Elisabetta;Battistini, Lucia;Curti, Claudio;Zanardi, Franca
;
Sartori, Andrea
2019

Abstract

We report here the preparation, physico-chemical characterization, and biological evaluation of a new liposome formulation as a tool for tumor angiogenesis inhibition. Liposomes are loaded with sunitinib, a tyrosine kinase inhibitor, and decorated with cyclo-aminoprolineRGD units (cAmpRGD), efficient and selective ligands for integrin α V β 3 . The RGD units play multiple roles since they target the nanovehicles at the integrin α V β 3 -overexpressing cells (e.g. activated endothelial cells), favor their active cell internalization, providing drug accumulation in the cytoplasm, and likely take part in the angiogenesis inhibition by interfering in the α V β 3 -VEGFR2 cross-talk. Both in vitro and in vivo studies show a better efficacy of this integrated antiangiogenic tool with respect to the free sunitinib and untargeted sunitinib-loaded liposomes. This system could allow a lower administration of the drug and, by increasing the vector specificity, reduce side-effects in a prolonged antiangiogenic therapy.
Integrin-targeted AmpRGD sunitinib liposomes as integrated antiangiogenic tools / Bianchini, Francesca; De Santis, Augusta; Portioli, Elisabetta; Russo Krauss, Irene; Battistini, Lucia; Curti, Claudio; Peppicelli, Silvia; Calorini, Lido; D'Errico, Gerardino; Zanardi, Franca; Sartori, Andrea. - In: NANOMEDICINE. - ISSN 1549-9634. - 18:(2019), pp. 135-145. [10.1016/j.nano.2019.02.015]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11381/2857865
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