Physicochemical characteristics of cationic vesicular systems prepared from biocompatible diacylglycerol-arginine surfactants are investigated. These systems form stable cationic vesicles by themselvesand the average diameter of the vesicles decreases as the alkyl chain length of the surfactant increases.The addition of DPPC also modifies the physicochemical properties of these vesicles. Among the drugsthese cationic formulations can encapsulate, we have considered Ciprofloxacin and 5-Fluorouracil (5-FU).We show that the percentage of encapsulated drug depends on both the physicochemical properties ofthe carrier and the type of drug. The capacity of these systems to carry different molecules was evaluatedperforming in vitro drug release studies. Finally, the antimicrobial activity of empty and Ciprofloxacin-loaded vesicles against Gram-positive and Gram-negative bacteria has been determined. Three bacteriawere tested: Escherichia coli, Staphylococcus aureus and Klebsiella pneumoniae. The in vitro drug releasefrom all formulations was effectively delayed. Empty cationic vesicles showed antimicrobial activity andCiprofloxacin-loaded vesicles showed similar or higher antimicrobial activity than the free drug solution.These results suggest that our formulations represent a great innovation in the pharmaceutical field, dueto their dual pharmacological function: one related to the nature of the vehiculated drug and the otherrelated to the innate antibacterial properties of the surfactant-based carriers.