Publication Type Journal Article
Title New iron(III) anti-cancer aminobisphenolate/phenanthroline complexes: Enhancing their therapeutic potential using nanoliposomes
Authors Cristina P. Matos Melissa Albino Joana Lopes Ana Silveira Viana Leonor Côrte-Real Filipa Mendes Joao Costa Pessca Ana Isabel Tomaz Catarina Pinto Reis M. Manuela Gaspar Isabel Correia
Groups BIOIN
Journal INTERNATIONAL JOURNAL OF PHARMACEUTICS
Year 2022
Month
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Volume 623
Number
Pages
Abstract Malignant melanoma is an aggressive and deadly form of skin cancer and novel and improved therapeutic options are needed. A promising strategy involves the use of metallodrugs combined with liposomes for targeted delivery to cancer cells. In this work, a family of iron(III) complexes was synthesized bearing a trianionic aminobisphenolate ligand (L) and phenanthroline-type co-ligands (NN). Four ternary iron complexes of general formula [Fe(L)(NN)] were obtained: [Fe(L)(amphen)] (1), [Fe(L)(phen)] (2), [Fe(L)(Clphen)] (3), and [Fe(L) (Mephen)] (4), as well as a fifth complex [Fe(L)(NEt3)(H2O)] (5) without the bidentate co-ligand. All complexes were characterized by analytic and spectroscopic techniques and demonstrated to be stable in aqueous environment. Complexes 1 and 2 were able to bind DNA and presented high cytotoxic activity towards human cancer cells. Complex 1 (IronC) was selected for incorporation into different liposomal formulations, which were fully characterized and screened against murine melanoma cells. The IronC liposomal formulation with the highest incorporation efficiency (similar to 95\%) and a low IC50 value (7.1 +/- 0.7 mu M) was selected for in vivo evaluation. In a syngeneic murine melanoma model the liposomal formulation of IronC yielded the highest impairment on tumour progression when compared with the control, temozolomide, and with the iron complex in free form.
DOI http://dx.doi.org/10.1016/j.ijpharm.2022.121925
ISBN
Publisher ELSEVIER
Book Title
ISSN 0378-5173
EISSN 1873-3476
Conference Name
Bibtex ID WOS:000828717100002
Observations
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