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Issue 9, 2015
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Inclusion of new 5-fluorouracil amphiphilic derivatives in liposome formulation for cancer treatment

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Abstract

5-Fluorouracil (5-FU) is widely employed in the treatment of some of the most frequently occurring malignant tumours such as breast, colon, and skin cancer. Unfortunately, 5-FU exhibits high toxicity and low tumor affinity with the risk of limited effectiveness and severe side effects for the patients. Numerous derivatives have been synthesized to improve the physicochemical, biopharmaceutical and pharmacokinetic properties of 5-FU, diminishing or circumventing some of its disadvantages. Three 4-substituted 5-fluoropyrimidines characterized by the presence of a polyoxyethylene chain of different lengths and a hydrophobic alkyl chain were synthesized and characterized. The new 5-FU derivatives were included in cationic liposomes formulated with a natural phospholipid and a cationic gemini surfactant to be delivered to cancer cells. The cytotoxicity of the formulations was evaluated by MTT assay on the HCT116 cancer cell line in vitro. The investigated liposome formulations showed a higher cytotoxicity compared to the free drug, thus showing great potential in cancer therapy.

Graphical abstract: Inclusion of new 5-fluorouracil amphiphilic derivatives in liposome formulation for cancer treatment

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Submitted
20 Feb 2015
Accepted
20 Jul 2015
First published
23 Jul 2015

Med. Chem. Commun., 2015,6, 1639-1642
Article type
Concise Article

Inclusion of new 5-fluorouracil amphiphilic derivatives in liposome formulation for cancer treatment

M. Petaccia, M. Condello, L. Giansanti, A. La Bella, F. Leonelli, S. Meschini, D. Gradella Villalva, E. Pellegrini, F. Ceccacci, L. Galantini and G. Mancini, Med. Chem. Commun., 2015, 6, 1639
DOI: 10.1039/C5MD00077G

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