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Title: Development of Pranoprofen Loaded Nanostructured Lipid Carriers to Improve Its Release and Therapeutic Efficacy in Skin Inflammatory Disorders
Author: Rincón, María
Calpena Campmany, Ana Cristina
Fábrega Fernández, María José
Garduño Ramírez, María Luisa del Carmen
Espina García, Marta
Rodríguez Lagunas, María José
García López, María Luisa
Abrego Escobar, Guadalupe
Keywords: Agents antiinflamatoris
Malalties de la pell
Administració de medicaments
Antiinflammatory agents
Skin diseases
Administration of drugs
Issue Date: 7-Dec-2018
Publisher: MDPI
Abstract: Abstract: Pranoprofen (PF)-loaded nanostructured lipid carriers (NLCs), prepared using a high-pressure homogenization method, have been optimized and characterized to improve the biopharmaceutical profile of the drug. The optimized PF-NLCs exhibited physicochemical characteristics and morphological properties that were suitable for dermal application. Stability assays revealed good physical stability, and the release behavior of PF from these NLCs showed a sustained release pattern. Cell viability results revealed no toxicity. Ex vivo human skin permeation studies in Franz diffusion cells were performed to determine the influence of different skin penetration enhancers (pyrrolidone, decanol, octanoic acid, nonane, menthone, squalene, linoleic acid, and cineol) on skin penetration and retention of PF, being the highest dermal retention in the presence of linoleic acid. The selected formulations of NLCs exhibited a high retained amount of PF in the skin and no systemic effects. In vivo mice anti-inflammatory efficacy studies showed a significant reduction in dermal oedema. NLCs containing linoleic acid presented better anti-inflammatory efficacy by decreasing the production of interleukins in keratinocytes and monocytes. The biomechanical properties of skin revealed an occlusive effect and no hydration power. No signs of skin irritancy in vivo were detected. According to these results, dermal PF-NLCs could be an effective system for the delivery and controlled release of PF, improving its dermal retention, with reduced dermal oedema as a possible effect of this drug KEYWORDS: anti-inflammatory activity; linoleic acid; nanostructured lipid carriers; penetration enhancers; pranoprofen; skin delivery
Note: Reproducció del document publicat a:
It is part of: Nanomaterials, 2018, vol. 8, num. 12, p. 1022-1050
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ISSN: 2079-4991
Appears in Collections:Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)
Articles publicats en revistes (Bioquímica i Fisiologia)

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