title: Cationic vesicles based on biocompatible diacyl glycerol-arginine surfactants: physicochemical properties, antimicrobial activity, encapsulation efficiency and drug release.
abstract: Physicochemical characteristics of cationic vesicular systems prepared from biocompatible diacyl glycerol-arginine surfactants are investigated. These systems form stable cationic vesicles by themselves and 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 drugs these 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 of the carrier and the type of drug. The capacity of these systems to carry different molecules was evaluated performing 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 bacteria were tested: Escherichia coli, Staphylococcus aureus and Klebsiella pneumoniae. The in vitro drug release from all formulations was effectively delayed. Empty cationic vesicles showed antimicrobial activity and Ciprofloxacin-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, due to their dual pharmacological function: one related to the nature of the vehiculated drug and the other related to the innate antibacterial properties of the surfactant-based carriers.
authors.affiliation: Department of Pharmacy, Health and Nutrition Sciences, University of Calabria, Edificio Polifunzionale, 87036 Arcavacata di Rende, Italy; Department of Engineering Modelling, University of Calabria, Via P. Bucci-Cubo 39C, 87036 Arcavacata di Rende, Italy.
authors.forename: L
authors.initials: L
authors.lastname: Tavano
authors.affiliation: Department of Chemical and Surfactants Technology, IQAC-CSIC, Jordi Girona 18-26, 08034 Barcelona, Spain.
authors.forename: A
authors.initials: A
authors.lastname: Pinazo
authors.affiliation: Chemistry Department, Faculty of Science, Benha University, Benha, Egypt.
authors.forename: M
authors.initials: M
authors.lastname: Abo-Riya
authors.affiliation: Department of Chemical and Surfactants Technology, IQAC-CSIC, Jordi Girona 18-26, 08034 Barcelona, Spain.
authors.forename: M R
authors.initials: MR
authors.lastname: Infante
authors.affiliation: Department of Microbiology, University of Barcelona, Joan XXIII s/n, 08028 Barcelona, Spain.
authors.forename: M A
authors.initials: MA
authors.lastname: Manresa
authors.affiliation: Department of Pharmacy, Health and Nutrition Sciences, University of Calabria, Edificio Polifunzionale, 87036 Arcavacata di Rende, Italy.
authors.forename: R
authors.initials: R
authors.lastname: Muzzalupo
authors.affiliation: Department of Chemical and Surfactants Technology, IQAC-CSIC, Jordi Girona 18-26, 08034 Barcelona, Spain. Electronic address: lpmste@cid.csic.es.
authors.forename: L
authors.initials: L
authors.lastname: Pérez
mesh_terms: D000890:Anti-Infective Agents / Q000737:chemistry / Q000494:pharmacology*; D001120:Arginine / Q000737:chemistry*; D001419:Bacteria / Q000187:drug effects; D001672:Biocompatible Materials / Q000737:chemistry*; D002412:Cations; D055598:Chemical Phenomena; D002939:Ciprofloxacin / Q000494:pharmacology; D004075:Diglycerides / Q000737:chemistry*; D065546:Drug Liberation; D005472:Fluorouracil / Q000494:pharmacology; D057446:Hydrodynamics; D006863:Hydrogen-Ion Concentration; D008081:Liposomes / Q000737:chemistry*; D008826:Microbial Sensitivity Tests; D010316:Particle Size; D055672:Static Electricity; D013501:Surface-Active Agents / Q000138:chemical synthesis / Q000737:chemistry*
chemical_list: C011439:1,2-diacylglycerol; D000890:Anti-Infective Agents; D001672:Biocompatible Materials; D002412:Cations; D004075:Diglycerides; D008081:Liposomes; D013501:Surface-Active Agents; D002939:Ciprofloxacin; D001120:Arginine; D005472:Fluorouracil
keywords: 5-Fluorouracil; Antimicrobial activity; Ciprofloxacin; Diacyl glycerol-arginine surfactants; Release; Vesicles