title: Physicochemical, cytotoxic, and dermal release features of a novel cationic liposome nanocarrier.
abstract: A novel cationic liposome nanocarrier, having interesting performance in topical drug delivery, is here presented and evaluated for its features. Two penetration enhancers, namely monoolein and lauroylcholine chloride, are combined to rapidly formulate (15 min) a cationic liposome nanostructure endowed of excellent stability (>6 months) and skin penetration ability, along with low short-term cytotoxicity, as evaluated via the MTT test. Cytotoxicity tests and lipid droplet analysis give a strong indication that monoolein and lauroylcholine synergistically endanger long-term cells viability. The physicochemical features, investigated through SAXS, DLS, and cryo-TEM techniques, reveal that the nanostructure is retained after loading with diclofenac in its acid (hydrophobic) form. The drug release performances are studied using intact newborn pig skin. Analysis of the different skin strata proves that the drug mainly accumulates into the viable epidermis with almost no deposition into the derma. Indeed, the flux of the drug across the skin is exceptionally low, with only 1% release after 24 h. These results validate the use of this novel formulation for topical drug release when the delivery to the systemic circulation should be avoided.
authors.affiliation: Department of Chemical and Geological Sciences, University of Cagliari, CNBS and CSGI, s.s. 554, bivio Sestu, 09042 Monserrato (CA), Italy.
authors.forename: Maura
authors.initials: M
authors.lastname: Carboni
authors.forename: Angela M
authors.initials: AM
authors.lastname: Falchi
authors.forename: Sandrina
authors.initials: S
authors.lastname: Lampis
authors.forename: Chiara
authors.initials: C
authors.lastname: Sinico
authors.forename: Maria L
authors.initials: ML
authors.lastname: Manca
authors.forename: Judith
authors.initials: J
authors.lastname: Schmidt
authors.forename: Yeshayahu
authors.initials: Y
authors.lastname: Talmon
authors.forename: Sergio
authors.initials: S
authors.lastname: Murgia
authors.forename: Maura
authors.initials: M
authors.lastname: Monduzzi
mesh_terms: D000287:Administration, Topical; D000818:Animals; D002412:Cations; D004008:Diclofenac / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D008081:Liposomes / Q000008:administration & dosage* / Q000737:chemistry* / Q000633:toxicity; D053769:Nanocapsules / Q000008:administration & dosage* / Q000737:chemistry* / Q000633:toxicity; D012869:Skin Absorption / Q000187:drug effects / Q000502:physiology*; D013552:Swine; D014018:Tissue Distribution
chemical_list: D002412:Cations; D008081:Liposomes; D053769:Nanocapsules; D004008:Diclofenac