title: Impact of lipid dynamic behavior on physical stability, in vitro release and skin permeation of genistein-loaded lipid nanoparticles.
abstract: The aim of this study was to develop lipid nanoparticles to deliver genistein (GEN) to deeper skin layers. To do so, the impact of lipid dynamic behavior (nanoparticle flexibility) on stability, release and skin permeation studies was verified. GEN-loaded solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) were obtained and characterization was undertaken. Freshly prepared nanoparticles were produced with similar features (i.e., drug loading). However, a higher level of crystallization in GEN-SLN formulation was observed in differential scanning calorimetry experiments. Electron paramagnetic resonance measurements showed a lower mobility of the spin labels in the SLN, which would indicate that NLC could be more flexible than SLN. Despite the fact that NLC demonstrated more fluidity, GEN was released more slowly from NLC than from SLN. Skin permeation studies demonstrated that lipid nanoparticles increased GEN skin retention. More flexible particles (NLC) also favored drug penetration into deeper skin layers. GEN-NLC would seem to be a promising formulation for GEN topical delivery.
authors.affiliation: Pharmaceutical Technology Laboratory, Universidade Federal de Goiás (UFG), Goiânia, Brazil.
authors.forename: Lígia Marquez
authors.initials: LM
authors.lastname: Andrade
authors.affiliation: Pharmaceutical Technology Laboratory, Universidade Federal de Goiás (UFG), Goiânia, Brazil.
authors.forename: Carolina
authors.initials: C
authors.lastname: de Fátima Reis
authors.affiliation: Pharmaceutical Technology Laboratory, Universidade Federal de Goiás (UFG), Goiânia, Brazil.
authors.forename: Lorena
authors.initials: L
authors.lastname: Maione-Silva
authors.affiliation: Physics Department, Universidade Federal de Goiás (UFG), Catalão, Brazil.
authors.forename: Jorge Luiz V
authors.initials: JL
authors.lastname: Anjos
authors.affiliation: Biophysics Laboratory, Universidade Federal de Goiás (UFG), Goiânia, Brazil.
authors.forename: Antonio
authors.initials: A
authors.lastname: Alonso
authors.affiliation: Pharmaceutical Technology Laboratory, Universidade Federal de Goiás (UFG), Goiânia, Brazil.
authors.forename: Rafael Caixeta
authors.initials: RC
authors.lastname: Serpa
authors.affiliation: Pharmaceutical Technology Laboratory, Universidade Federal de Goiás (UFG), Goiânia, Brazil.
authors.forename: Ricardo Neves
authors.initials: RN
authors.lastname: Marreto
authors.affiliation: Pharmaceutical Technology Laboratory, Universidade Federal de Goiás (UFG), Goiânia, Brazil.
authors.forename: Eliana Martins
authors.initials: EM
authors.lastname: Lima
authors.affiliation: Pharmaceutical Technology Laboratory, Universidade Federal de Goiás (UFG), Goiânia, Brazil. Electronic address: stephaniafleury@ufg.com.br.
authors.forename: Stephânia Fleury
authors.initials: SF
authors.lastname: Taveira
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers / Q000737:chemistry; D004431:Ear, External / Q000187:drug effects; D004578:Electron Spin Resonance Spectroscopy; D019833:Genistein / Q000008:administration & dosage*; D008055:Lipids / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D012867:Skin / Q000187:drug effects*; D012869:Skin Absorption; D013552:Swine
chemical_list: D004337:Drug Carriers; D008055:Lipids; D019833:Genistein
keywords: Characterization; Electron paramagnetic resonance; Flexibility; Genistein; Lipid dynamic; Nanostructured lipid carriers; Skin permeation; Solid lipid nanoparticles; Stability