title: Formulation strategies to modulate the topical delivery of anti-inflammatory compounds.
abstract: The aim of this study was to assess the ability of some vehicles (emulsion and emulgel), containing hydrogenated lecithin as penetration enhancer, in increasing the percutaneous absorption of the two model compounds dipotassium glycyrrhizinate (DG) and stearyl glycyrrhetinate (SG). Furthermore SG-loaded solid lipid nanoparticles (SLNs) were prepared and the effect of this vehicle on SG permeation profile was evaluated as well. Percutaneous absorption has been studied in vitro, using excised human skin membranes (i.e., stratum corneum epidermis or [SCE]), and in vivo, determining their anti-inflammatory activity. From the results obtained, the use of both penetration enhancers and SLNs resulted in being valid tools to optimize the topical delivery of DG and SG. Soy lecithin guaranteed an increase in the percutaneous absorption of the two activities and a rapid anti-inflammatory effect in in vivo experiments, whereas SLNs produced an interesting delayed and sustained release of SG.
authors.affiliation: Department of Drug Sciences, University of Catania, 95125 Catania (C.P., L.R., A.O., F.B.), and R&D, Rottapharm|Madaus, Monza (F.G., V.G.), Italy.
authors.forename: Carmelo
authors.initials: C
authors.lastname: Puglia
authors.forename: Luisa
authors.initials: L
authors.lastname: Rizza
authors.forename: Alessia
authors.initials: A
authors.lastname: Offerta
authors.forename: Franco
authors.initials: F
authors.lastname: Gasparri
authors.forename: Valentina
authors.initials: V
authors.lastname: Giannini
authors.forename: Francesco
authors.initials: F
authors.lastname: Bonina
mesh_terms: D000287:Administration, Topical; D000328:Adult; D000893:Anti-Inflammatory Agents / Q000378:metabolism / Q000494:pharmacology*; D004337:Drug Carriers; D004655:Emulsions; D004890:Erythema / Q000188:drug therapy / Q000209:etiology / Q000473:pathology; D005260:Female; D005782:Gels; D006034:Glycyrrhetinic Acid / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D019695:Glycyrrhizic Acid / Q000378:metabolism / Q000494:pharmacology*; D006801:Humans; D006865:Hydrogenation; D054709:Lecithins / Q000378:metabolism*; D008297:Male; D053758:Nanoparticles; D010316:Particle Size; D010539:Permeability; D012867:Skin / Q000187:drug effects / Q000378:metabolism / Q000473:pathology; D012869:Skin Absorption; D014466:Ultraviolet Rays / Q000009:adverse effects
chemical_list: D000893:Anti-Inflammatory Agents; D004337:Drug Carriers; D004655:Emulsions; D005782:Gels; D054709:Lecithins; C013689:stearyl glycyrrhetinate; D019695:Glycyrrhizic Acid; D006034:Glycyrrhetinic Acid