title: Effect of lipid nanoparticle formulations on skin delivery of a lipophilic substance.
abstract: The aim of this study was to follow the skin penetration of a model lipophilic compound (Nile red) delivered by nanoparticulate carriers, the so-called lipid nanocapsules. The nanocapsules consisting of an oil core stabilized by amixture of surfactants were prepared by the phase inversion temperature method. Varying the particle composition (the oil/surfactant ratio) nanoparticles of different size were prepared and characterized. The penetration profile of Nile red delivered into the porcine skin by the nanoparticles compared to non-particulate samples was determined using fluorescence microscopy combined with a novel, statistically robust quantitative image analysis method. This study demonstrated that lipid nanoparticles promoted the skin penetration of encapsulated Nile red in comparison with all the non-particulate samples. Nile red delivered by the lipid-based nanoparticles was able to diffuse across the stratum corneum and partition itself uniformly in the epidermis. No relationship between Nile red penetration into the skin and the particle size was found. Moreover, the presence of sodium chloride in the water phase had a negative impact on the Nile red penetration into the skin. The results indicate that the physico-chemical circumstances of the nanoparticulate formulation play the major role in the penetration of lipophilic substances into the skin.
authors.affiliation: Department of Chemical Engineering, University of Chemistry and Technology Prague, Technická 3, 166 28 Prague 6, Czech Republic.
authors.forename: Lucie
authors.initials: L
authors.lastname: Vidlářová
authors.affiliation: Department of Chemical Engineering, University of Chemistry and Technology Prague, Technická 3, 166 28 Prague 6, Czech Republic.
authors.forename: Jaroslav
authors.initials: J
authors.lastname: Hanuš
authors.affiliation: Department of Organic Technology, University of Chemistry and Technology Prague, Technická 3, 166 28 Prague 6, Czech Republic.
authors.forename: Martin
authors.initials: M
authors.lastname: Veselý
authors.affiliation: Department of Biochemistry and Microbiology, University of Chemistry and Technology Prague, Technická 3, 166 28 Prague 6, Czech Republic.
authors.forename: Pavel
authors.initials: P
authors.lastname: Ulbrich
authors.affiliation: Department of Chemical Engineering, University of Chemistry and Technology Prague, Technická 3, 166 28 Prague 6, Czech Republic. Electronic address: Frantisek.Stepanek@vscht.cz.
authors.forename: František
authors.initials: F
authors.lastname: Štěpánek
authors.affiliation: Department of Organic Technology, University of Chemistry and Technology Prague, Technická 3, 166 28 Prague 6, Czech Republic; Department of Pharmaceutical Technology, Faculty of Pharmacy in Hradec Králové, Charles University in Prague, Heyrovského 1203, 50005 Hradec Králové, Czech Republic. Electronic address: Jarmila.Zbytovska@vscht.cz.
authors.forename: Jarmila
authors.initials: J
authors.lastname: Zbytovská
mesh_terms: D000818:Animals; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D004817:Epidermis / Q000187:drug effects*; D007091:Image Processing, Computer-Assisted; D008055:Lipids / Q000737:chemistry*; D018613:Microscopy, Confocal; D046529:Microscopy, Electron, Transmission; D008856:Microscopy, Fluorescence; D053769:Nanocapsules / Q000737:chemistry; D053758:Nanoparticles / Q000737:chemistry*; D009821:Oils / Q000737:chemistry; D010078:Oxazines / Q000737:chemistry; D010316:Particle Size; D012867:Skin / Q000187:drug effects / Q000473:pathology; D012869:Skin Absorption; D012984:Software; D013501:Surface-Active Agents / Q000737:chemistry; D013552:Swine
chemical_list: D004337:Drug Carriers; D008055:Lipids; D053769:Nanocapsules; D009821:Oils; D010078:Oxazines; D013501:Surface-Active Agents; C044808:nile red
keywords: Image analysis; Lipid nanoparticles; Nile red; Phase inversion temperature method; Skin penetration