Development of pranoprofen loaded nanostructured lipid carriers to improve its release and therapeutic efficacy in skin inflammatory disorders
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- dc.contributor.author Rincón, María
- dc.contributor.author Calpena, Ana C.
- dc.contributor.author Fábrega, María José
- dc.contributor.author Garduño-Ramírez, María L.
- dc.contributor.author Espina, Marta
- dc.contributor.author Rodríguez-Lagunas, María J.
- dc.contributor.author García, María L.
- dc.contributor.author Abrego, Guadalupe
- dc.date.accessioned 2022-10-18T08:48:54Z
- dc.date.available 2022-10-18T08:48:54Z
- dc.date.issued 2018
- dc.description Includes supplementary materials for the online appendix.
- dc.description.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.
- dc.description.sponsorship This work was supported by the Spanish Ministry of Science and Innovation (MAT2014-59134-R projects). The authors would like to thank the University of Barcelona for the financial support to cover the cost of open access publication. María Rincón would like to thank M. Silva-Abreu, L. Halbaut and L.M. Rincón for their technical support.
- dc.format.mimetype application/pdf
- dc.identifier.citation Rincón M, Calpena AC, Fabrega MJ, Garduño-Ramírez ML, Espina M, Rodríguez-Lagunas MJ, et al. Development of pranoprofen loaded nanostructured lipid carriers to improve its release and therapeutic efficacy in skin inflammatory disorders. Nanomaterials. 2018 Dec 7;8(12):1-28. DOI: 10.3390/nano8121022
- dc.identifier.doi http://dx.doi.org/10.3390/nano8121022
- dc.identifier.issn 2079-4991
- dc.identifier.uri http://hdl.handle.net/10230/54462
- dc.language.iso eng
- dc.publisher MDPI
- dc.relation.ispartof Nanomaterials. 2018 Dec 7;8(12):1-28
- dc.relation.projectID info:eu-repo/grantAgreement/ES/1PE/MAT2014-59134-R
- dc.rights © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
- dc.rights.accessRights info:eu-repo/semantics/openAccess
- dc.rights.uri http://creativecommons.org/licenses/by/4.0/
- dc.subject.keyword Pranoprofen
- dc.subject.keyword Nanostructured lipid carriers
- dc.subject.keyword Penetration enhancers
- dc.subject.keyword Linoleic acid
- dc.subject.keyword Skin delivery
- dc.subject.keyword Anti-inflammatory activity
- dc.title Development of pranoprofen loaded nanostructured lipid carriers to improve its release and therapeutic efficacy in skin inflammatory disorders
- dc.type info:eu-repo/semantics/article
- dc.type.version info:eu-repo/semantics/publishedVersion