Nanoformulations of a potent copper-based aquaporin inhibitor with cytotoxic effect against cancer cells

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Nanoformulations of a potent copper-based aquaporin inhibitor with cytotoxic effect against cancer cells

Monday, 01.08.2016

Authors and Affiliations:

Mariana Navea, Rui E. Castroa, Cecília M. P. Rodriguesa, Angela Casinib, Graça Soverala, M. Manuela Gaspara

a Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Av. Prof. Gama Pinto, 1649-003, Lisboa, Portugal

b School of Chemistry, Cardiff University, Park Place, Cardiff CF 10 3AT, United Kingdom

 

Abstract:

Aim: development of liposomal formulations of Cuphen, a potent copper-based aquaporin inhibitor with therapeutic potential against melanoma and colon cancer.

Materials & Methods: Cuphen was incorporated into liposomes using de-hydration re-hydration method. The ability of Cuphen to induce cell death was evaluated by MTS and ViaCount assays. In vivo toxicity studies were performed in BALB/c mice.

Results: In vitro studies illustrated the antiproliferative effects of Cuphen in different cancer cell lines, in free form or after incorporation into liposomes. In vivo studies revealed no toxic effects after parenteral administration of Cuphen liposomes.

Conclusions: Cuphen liposomes are highly attractive to be further tested in murine models due to the possibility of stabilizing and specifically deliver this metallodrug to tumor sites.

  

Journal: Nanomedicine

 

Link: http://www.futuremedicine.com/doi/10.2217/nnm-2016-0086