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 |
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Pages |
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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 |
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Publisher |
ELSEVIER |
Book Title |
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ISSN |
0378-5173 |
EISSN |
1873-3476 |
Conference Name |
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Bibtex ID |
WOS:000828717100002 |
Observations |
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