title: Improving ex vivo skin permeation of non-steroidal anti-inflammatory drugs: enhancing extemporaneous transformation of liposomes into planar lipid bilayers.
abstract: Transdermal delivery of active principles is a versatile method widely used in medicine. The main drawback for the transdermal route, however, is the low efficiency achieved in the absorption of many drugs, mostly due to the complexity of the skin barrier. To improve drug delivery through the skin, we prepared and characterized liposomes loaded with ibuprofen and designed pharmaceutical formulations based on the extemporaneous addition of penetration enhancer (PE) surfactants. Afterwards, permeation and release studies were carried out. According to the permeation studies, the ibuprofen liposomal formulation supplemented with PEs exhibited similar therapeutic effects, but at lower doses (20%) comparing with a commercial formulation used as a reference. Atomic force microscopy (AFM) was used to investigate the effect caused by PEs on the adsorption mechanism of liposomal formulations onto the skin. Non-fused liposomes, bilayers and multilayered lipid structures were observed. The transformation of vesicles into planar structures is proposed as a possible rationale for explaining the lower doses required when a liposome formulation is supplemented with surfactant PEs.
authors.affiliation: Departament de Fisicoquímica, Universitat de Barcelona, Av. Joan XXIII, 08028 Barcelona, Spain; Labiana Pharmaceuticals S.L.U., c/ Casanova 27-31, 08757 Corbera de Llobregat, Barcelona, Spain.
authors.forename: Martha L
authors.initials: ML
authors.lastname: Vázquez-González
authors.affiliation: Labiana Pharmaceuticals S.L.U., c/ Casanova 27-31, 08757 Corbera de Llobregat, Barcelona, Spain.
authors.forename: Rafael
authors.initials: R
authors.lastname: Bernad
authors.affiliation: Unitat de Farmàcia i Farmacocinètica, Facultat de Farmàcia, Universitat de Barcelona, Av. Joan XXIII, 08028 Barcelona, Spain; Institut de Nanociència i Nanotecnologia (IN(2)UB), Av. Joan XXIII, 08028 Barcelona, Spain.
authors.forename: Ana C
authors.initials: AC
authors.lastname: Calpena
authors.affiliation: Departament de Fisicoquímica, Universitat de Barcelona, Av. Joan XXIII, 08028 Barcelona, Spain; Institut de Nanociència i Nanotecnologia (IN(2)UB), Av. Joan XXIII, 08028 Barcelona, Spain.
authors.forename: Oscar
authors.initials: O
authors.lastname: Domènech
authors.affiliation: Departament de Fisicoquímica, Universitat de Barcelona, Av. Joan XXIII, 08028 Barcelona, Spain; Institut de Nanociència i Nanotecnologia (IN(2)UB), Av. Joan XXIII, 08028 Barcelona, Spain.
authors.forename: M T
authors.initials: MT
authors.lastname: Montero
authors.affiliation: Departament de Fisicoquímica, Universitat de Barcelona, Av. Joan XXIII, 08028 Barcelona, Spain; Institut de Nanociència i Nanotecnologia (IN(2)UB), Av. Joan XXIII, 08028 Barcelona, Spain. Electronic address: Jordiborrell@ub.edu.
authors.forename: Jordi
authors.initials: J
authors.lastname: Hernández-Borrell
mesh_terms: D000279:Administration, Cutaneous; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical / Q000379:methods; D016503:Drug Delivery Systems; D005260:Female; D006801:Humans; D007052:Ibuprofen / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008051:Lipid Bilayers / Q000378:metabolism; D008081:Liposomes; D018625:Microscopy, Atomic Force; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D013501:Surface-Active Agents / Q000737:chemistry
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D008051:Lipid Bilayers; D008081:Liposomes; D013501:Surface-Active Agents; D007052:Ibuprofen
keywords: AFM; Enhancers; Ibuprofen; Ibuprofen (PubChem CID: 3672); Liposomes; Transdermal drug delivery