title: In vitro and in vivo evaluation of a desonide gel-cream photostabilized with benzophenone-3.
abstract: BACKGROUND
  Our group previously reported the photoinstability of some desonide topical commercial formulations under direct exposure to UVA radiation.
  
  
  OBJECTIVE
  This study aimed to prepare and characterize a gel-cream containing desonide, with greater photostability than the commercial gel-cream (C-GC). Benzophenone-3 (BP-3) was used as a photostabilizing agent.
  
  
  METHODS
  The gel-cream developed (D-GC) containing BP-3 at 0.1% was prepared and characterized regarding its pH, drug content, spreadability, viscosity, in vitro drug release and in vitro permeation. The in vivo anti-inflammatory effect was assessed by ear edema measurement, croton oil-induced acute skin inflammation and myeloperoxidase assay.
  
  
  CONCLUSIONS
  D-GC presented characteristics compatible with topical application, appropriate drug content and good spreadability, and non-Newtonian behavior with pseudoplastic flow. D-GC showed a good photostability profile, presenting a desonide content of 95.70% after 48 h of exposure to UVA radiation, and stability under room conditions during 60 days. The amount of desonide released from D-GC and C-GC was 57.8 and 51.7 µg/cm2, respectively, measured using the vertical Franz cell. The in vitro skin permeation showed that desonide reached the site of action of the topical corticosteroids, from both formulations; however, the desonide amount retained in the dermis was lower with D-GC. The in vivo evaluation of topical anti-inflammatory activity indicated that D-GC presented the same biological effect as C-GC.
  
  
  CONCLUSIONS
  D-GC represents a promising approach to treat dermatological disorders, since it presented satisfactory physicochemical characteristics, the same biological activity as C-GC and superior photostability, conferred by the addition of BP-3 at 0.1%.
authors.affiliation: a Programa de Pós-Graduação em Ciências Farmacêuticas.
authors.forename: Priscila
authors.initials: P
authors.lastname: Rosa
authors.affiliation: b Departamento de Farmácia Industrial.
authors.forename: Juliana Dos
authors.initials: JD
authors.lastname: Santos
authors.affiliation: b Departamento de Farmácia Industrial.
authors.forename: Tássia Fontana
authors.initials: TF
authors.lastname: Lehmen
authors.affiliation: a Programa de Pós-Graduação em Ciências Farmacêuticas.
authors.forename: Julia
authors.initials: J
authors.lastname: Weber
authors.affiliation: a Programa de Pós-Graduação em Ciências Farmacêuticas.
authors.forename: Fernanda Cramer
authors.initials: FC
authors.lastname: Flores
authors.affiliation: b Departamento de Farmácia Industrial.
authors.forename: Cristiane de Bona da
authors.initials: CB
authors.lastname: Silva
authors.affiliation: c Departamento de Química , and.
authors.forename: Sara Marchesan
authors.initials: SM
authors.lastname: Oliveira
authors.affiliation: d Programa de Pós-Graduação em Ciências Biológicas: Bioquímica Toxicológica, Universidade Federal de Santa Maria , Santa Maria , Brazil.
authors.forename: Indiara
authors.initials: I
authors.lastname: Brusco
authors.affiliation: b Departamento de Farmácia Industrial.
authors.forename: Géssica Brum
authors.initials: GB
authors.lastname: Milani
authors.affiliation: b Departamento de Farmácia Industrial.
authors.forename: Andréa Inês Horn
authors.initials: AI
authors.lastname: Adams
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000494:pharmacology; D001577:Benzophenones / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D003436:Croton Oil / Q000633:toxicity; D003877:Dermatitis, Contact / Q000188:drug therapy*; D003879:Dermatologic Agents / Q000737:chemistry / Q000494:pharmacology; D003898:Desonide / Q000737:chemistry* / Q000494:pharmacology*; D004195:Disease Models, Animal; D004423:Ear; D005782:Gels; D005938:Glucocorticoids / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008297:Male; D051379:Mice; D012867:Skin / Q000187:drug effects; D063465:Skin Cream / Q000737:chemistry / Q000494:pharmacology; D014466:Ultraviolet Rays
chemical_list: D000893:Anti-Inflammatory Agents; D001577:Benzophenones; D003879:Dermatologic Agents; D005782:Gels; D005938:Glucocorticoids; D003436:Croton Oil; C005290:oxybenzone; D003898:Desonide
keywords: Benzophenone-3; MPO activity; corticosteroids photostability; desonide; ear edema; photostability; skin permeation