Cargando…

Omega-3- and Resveratrol-Loaded Lipid Nanosystems for Potential Use as Topical Formulations in Autoimmune, Inflammatory, and Cancerous Skin Diseases

Resveratrol (RSV) and omega 3 (ω(3)), because of their biological favorable properties, have become subjects of interest for researchers in dermocosmetic and pharmaceutical industries; however, these bioactives present technological limitations that hinder their effective delivery to the target skin...

Descripción completa

Detalles Bibliográficos
Autores principales: Caldas, Ana R., Catita, José, Machado, Raul, Ribeiro, Artur, Cerqueira, Fátima, Horta, Bruno, Medeiros, Rui, Lúcio, Marlene, Lopes, Carla M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8401194/
https://www.ncbi.nlm.nih.gov/pubmed/34452163
http://dx.doi.org/10.3390/pharmaceutics13081202
_version_ 1783745493552070656
author Caldas, Ana R.
Catita, José
Machado, Raul
Ribeiro, Artur
Cerqueira, Fátima
Horta, Bruno
Medeiros, Rui
Lúcio, Marlene
Lopes, Carla M.
author_facet Caldas, Ana R.
Catita, José
Machado, Raul
Ribeiro, Artur
Cerqueira, Fátima
Horta, Bruno
Medeiros, Rui
Lúcio, Marlene
Lopes, Carla M.
author_sort Caldas, Ana R.
collection PubMed
description Resveratrol (RSV) and omega 3 (ω(3)), because of their biological favorable properties, have become subjects of interest for researchers in dermocosmetic and pharmaceutical industries; however, these bioactives present technological limitations that hinder their effective delivery to the target skin layer. To overcome the stability and skin permeation limitations of free bioactives, this work proposes a combined strategy involving two different lipid nanosystems (liposomes and lipid nanoparticles) that include ω(3) in their lipid matrix. Additionaly, RSV is only encapsulated in liposomes that provid an adequate amphiphilic environment. Each formulation is thoroughly characterized regarding their physical–chemical properties. Subsequently, the therapeutic performance of the lipid nanosystems is evaluated based on their protective roles against lipid peroxidation, as well as inhibition of cicloxygenase (COX) and nitric oxid (NO) production in the RWA264.7 cell line. Finally, the lipid nanosystems are incorporated in hydrogel to allow their topical administration, then rheology, occlusion, and RSV release–diffusion assays are performed. Lipid nanoparticles provide occlusive effects at the skin surface. Liposomes provide sustained RSV release and their flexibility conferred by edge activator components enhances RSV diffusion, which is required to reach NO production cells and COX cell membrane enzymes. Overall, the inclusion of both lipid nanosystems in the same semisolid base constitutes a promising strategy for autoimmune, inflammatory, and cancerous skin diseases.
format Online
Article
Text
id pubmed-8401194
institution National Center for Biotechnology Information
language English
publishDate 2021
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-84011942021-08-29 Omega-3- and Resveratrol-Loaded Lipid Nanosystems for Potential Use as Topical Formulations in Autoimmune, Inflammatory, and Cancerous Skin Diseases Caldas, Ana R. Catita, José Machado, Raul Ribeiro, Artur Cerqueira, Fátima Horta, Bruno Medeiros, Rui Lúcio, Marlene Lopes, Carla M. Pharmaceutics Article Resveratrol (RSV) and omega 3 (ω(3)), because of their biological favorable properties, have become subjects of interest for researchers in dermocosmetic and pharmaceutical industries; however, these bioactives present technological limitations that hinder their effective delivery to the target skin layer. To overcome the stability and skin permeation limitations of free bioactives, this work proposes a combined strategy involving two different lipid nanosystems (liposomes and lipid nanoparticles) that include ω(3) in their lipid matrix. Additionaly, RSV is only encapsulated in liposomes that provid an adequate amphiphilic environment. Each formulation is thoroughly characterized regarding their physical–chemical properties. Subsequently, the therapeutic performance of the lipid nanosystems is evaluated based on their protective roles against lipid peroxidation, as well as inhibition of cicloxygenase (COX) and nitric oxid (NO) production in the RWA264.7 cell line. Finally, the lipid nanosystems are incorporated in hydrogel to allow their topical administration, then rheology, occlusion, and RSV release–diffusion assays are performed. Lipid nanoparticles provide occlusive effects at the skin surface. Liposomes provide sustained RSV release and their flexibility conferred by edge activator components enhances RSV diffusion, which is required to reach NO production cells and COX cell membrane enzymes. Overall, the inclusion of both lipid nanosystems in the same semisolid base constitutes a promising strategy for autoimmune, inflammatory, and cancerous skin diseases. MDPI 2021-08-04 /pmc/articles/PMC8401194/ /pubmed/34452163 http://dx.doi.org/10.3390/pharmaceutics13081202 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Caldas, Ana R.
Catita, José
Machado, Raul
Ribeiro, Artur
Cerqueira, Fátima
Horta, Bruno
Medeiros, Rui
Lúcio, Marlene
Lopes, Carla M.
Omega-3- and Resveratrol-Loaded Lipid Nanosystems for Potential Use as Topical Formulations in Autoimmune, Inflammatory, and Cancerous Skin Diseases
title Omega-3- and Resveratrol-Loaded Lipid Nanosystems for Potential Use as Topical Formulations in Autoimmune, Inflammatory, and Cancerous Skin Diseases
title_full Omega-3- and Resveratrol-Loaded Lipid Nanosystems for Potential Use as Topical Formulations in Autoimmune, Inflammatory, and Cancerous Skin Diseases
title_fullStr Omega-3- and Resveratrol-Loaded Lipid Nanosystems for Potential Use as Topical Formulations in Autoimmune, Inflammatory, and Cancerous Skin Diseases
title_full_unstemmed Omega-3- and Resveratrol-Loaded Lipid Nanosystems for Potential Use as Topical Formulations in Autoimmune, Inflammatory, and Cancerous Skin Diseases
title_short Omega-3- and Resveratrol-Loaded Lipid Nanosystems for Potential Use as Topical Formulations in Autoimmune, Inflammatory, and Cancerous Skin Diseases
title_sort omega-3- and resveratrol-loaded lipid nanosystems for potential use as topical formulations in autoimmune, inflammatory, and cancerous skin diseases
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8401194/
https://www.ncbi.nlm.nih.gov/pubmed/34452163
http://dx.doi.org/10.3390/pharmaceutics13081202
work_keys_str_mv AT caldasanar omega3andresveratrolloadedlipidnanosystemsforpotentialuseastopicalformulationsinautoimmuneinflammatoryandcancerousskindiseases
AT catitajose omega3andresveratrolloadedlipidnanosystemsforpotentialuseastopicalformulationsinautoimmuneinflammatoryandcancerousskindiseases
AT machadoraul omega3andresveratrolloadedlipidnanosystemsforpotentialuseastopicalformulationsinautoimmuneinflammatoryandcancerousskindiseases
AT ribeiroartur omega3andresveratrolloadedlipidnanosystemsforpotentialuseastopicalformulationsinautoimmuneinflammatoryandcancerousskindiseases
AT cerqueirafatima omega3andresveratrolloadedlipidnanosystemsforpotentialuseastopicalformulationsinautoimmuneinflammatoryandcancerousskindiseases
AT hortabruno omega3andresveratrolloadedlipidnanosystemsforpotentialuseastopicalformulationsinautoimmuneinflammatoryandcancerousskindiseases
AT medeirosrui omega3andresveratrolloadedlipidnanosystemsforpotentialuseastopicalformulationsinautoimmuneinflammatoryandcancerousskindiseases
AT luciomarlene omega3andresveratrolloadedlipidnanosystemsforpotentialuseastopicalformulationsinautoimmuneinflammatoryandcancerousskindiseases
AT lopescarlam omega3andresveratrolloadedlipidnanosystemsforpotentialuseastopicalformulationsinautoimmuneinflammatoryandcancerousskindiseases