title: Dithranol-loaded lipid-core nanocapsules improve the photostability and reduce the in vitro irritation potential of this drug.
abstract: Dithranol is a very effective drug for the topical treatment of psoriasis. However, it has some adverse effects such as irritation and stain in the skin that make its application and patient adherence to treatment difficult. The aims of this work were to prepare and characterize dithranol-loaded nanocapsules as well as to evaluate the photostability and the irritation potential of these nanocarriers. Lipid-core nanocapsules containing dithranol (0.5 mg/mL) were prepared by interfacial deposition of preformed polymer. EDTA (0.05%) or ascorbic acid (0.02%) was used as antioxidants. After preparation, dithranol-loaded lipid-core nanocapsules showed satisfactory characteristics: drug content close to the theoretical concentration, encapsulation efficiency of about 100%, nanometric mean size (230-250 nm), polydispersity index below 0.25, negative zeta potential, and pH values from 4.3 to 5.6. In the photodegradation study against UVA light, we observed a higher stability of the dithranol-loaded lipid-core nanocapsules comparing to the solution containing the free drug (half-life times around 4 and 1h for the dithranol-loaded lipid-core nanocapsules and free drug solution containing EDTA, respectively; half-life times around 17 and 7h for the dithranol-loaded lipid-core nanocapsules and free drug solution containing ascorbic acid, respectively). Irritation test by HET-CAM method was conducted to evaluate the safety of the formulations. From the results it was found that the nanoencapsulation of the drug decreased its toxicity compared to the effects observed for the free drug.
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal de Santa Maria, Av. Roraima, 1000, Santa Maria, RS 97105-900, Brazil.
authors.forename: Ana L
authors.initials: AL
authors.lastname: Savian
authors.affiliation: Curso de Farmácia, Centro de Ciências da Saúde, Universidade Federal de Santa Maria, Av. Roraima, 1000, Santa Maria, RS 97105-900, Brazil.
authors.forename: Daiane
authors.initials: D
authors.lastname: Rodrigues
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal de Santa Maria, Av. Roraima, 1000, Santa Maria, RS 97105-900, Brazil.
authors.forename: Julia
authors.initials: J
authors.lastname: Weber
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal de Santa Maria, Av. Roraima, 1000, Santa Maria, RS 97105-900, Brazil.
authors.forename: Roseane F
authors.initials: RF
authors.lastname: Ribeiro
authors.affiliation: Curso de Farmácia, Centro de Ciências da Saúde, Universidade Federal de Santa Maria, Av. Roraima, 1000, Santa Maria, RS 97105-900, Brazil.
authors.forename: Mariana H
authors.initials: MH
authors.lastname: Motta
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal de Santa Maria, Av. Roraima, 1000, Santa Maria, RS 97105-900, Brazil.
authors.forename: Scheila R
authors.initials: SR
authors.lastname: Schaffazick
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal de Santa Maria, Av. Roraima, 1000, Santa Maria, RS 97105-900, Brazil.
authors.forename: Andréa I H
authors.initials: AI
authors.lastname: Adams
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, Porto Alegre, RS 90610-000, Brazil.
authors.forename: Diego F
authors.initials: DF
authors.lastname: de Andrade
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, Porto Alegre, RS 90610-000, Brazil.
authors.forename: Ruy C R
authors.initials: RC
authors.lastname: Beck
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal de Santa Maria, Av. Roraima, 1000, Santa Maria, RS 97105-900, Brazil. Electronic address: csbona@smail.ufsm.br.
authors.forename: Cristiane B
authors.initials: CB
authors.lastname: da Silva
mesh_terms: D000818:Animals; D000875:Anthralin / Q000737:chemistry* / Q000493:pharmacokinetics / Q000633:toxicity; D002626:Chemistry, Pharmaceutical; D002642:Chick Embryo; D002645:Chickens; D049033:Chorioallantoic Membrane / Q000187:drug effects; D003879:Dermatologic Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000633:toxicity; D004337:Drug Carriers / Q000737:chemistry* / Q000633:toxicity; D004355:Drug Stability; D008055:Lipids / Q000737:chemistry* / Q000633:toxicity; D053769:Nanocapsules / Q000737:chemistry* / Q000633:toxicity; D010782:Photolysis
chemical_list: D003879:Dermatologic Agents; D004337:Drug Carriers; D008055:Lipids; D053769:Nanocapsules; D000875:Anthralin
keywords: Dithranol; Irritation potential; Lipid-core nanocapsules; Photostability