Pyrene lipids are useful tools to investigate membrane organization and intracellular lipid trafficking. The molecular interactions controlling the organization of lipid monolayers composed of a cationic amphiphile tagged with a pyrene residue and a saturated or unsaturated phospholipid, namely, 1,2-dimyristoyl-sn-glycero-3-phosphocholine and 1,2-dioleoyl-sn-glycero-3-phosphocholine, were investigated by Langmuir trough isotherms to understand how the molecular structure of the components and their relative amount affect the physicochemical properties of lipid monolayers. The obtained results show that the cationic headgroups and unsaturation of hydrophobic chains strongly affect the organization of the lipid monolayer as a function of the amount of components. On the other hand, the presence of the pyrene moiety does not seem to have a marked influence on the interaction within lipid assembly.

No 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

No abstract