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; G. Mancini

doi:10.1039/C5MD00077G

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

M. Petaccia,‡^a M. Condello,‡^bc L. Giansanti,^a A. La Bella,^d F. Leonelli,^e S. Meschini,*^b D. Gradella Villalva,^d E. Pellegrini,^b F. Ceccacci,^f L. Galantini^d and G. Mancini*^c

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* Corresponding authors

^a Dipartimento di Scienze Fisiche e Chimiche, Università degli Studi dell'Aquila, Via Vetoio 67100 Coppito (Aq), Italy

^b Dipartimento Tecnologie e Salute, Istituto Superiore di Sanità, Viale Regina Elena 299, 00161 Roma, Italy
E-mail: stefania.meschini@iss.it
Fax: +390649903563
Tel: +390649902783

^c CNR – Istituto di Metodologie Chimiche, Via Salaria km 29.300, 00016 Monterotondo Scalo (RM), Italy
E-mail: giovanna.mancini@uniroma1.it
Fax: +390649913629
Tel: +390690625111

^d Dipartimento di Chimica, Università degli Studi di Roma “Sapienza”, P.le Aldo Moro 5, 00185 Roma, Italy

^e Dipartimento di Biologia Vegetale ed Animale, Università degli Studi di Roma “Sapienza”, P.le Aldo Moro 5, 00185 Roma, Italy

^f CNR-IMC, Sezione Meccanismi di Reazione c/o Dipartimento di Chimica, Università degli Studi di Roma “Sapienza”, P.le Aldo Moro 5, 00185 Roma, Italy

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.

MedChemComm

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

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

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