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 (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 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 physicalchemical 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 releasediffusion 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.
This research was funded by FCT/MCTES—Foundation for Science and Technology I.P. from the Minister of Science, Technology, and Higher Education (PIDDAC) and European Regional Development Fund (ERDF) by the COMPETE—Programa Operacional Factores de Competitividade (POFC) through the project CONCERT (POCI-01-0145-FEDER-032651 and PTDC/NAN-MAT/326512017) and the Strategic Funding UID/Multi/04546/2019, UIDP/04423/2020 (Group of Natural Products and Medicinal Chemistry CIIMAR), and “Contrato-Programa” UIDB/04469/2020 (CF-UM-UP) and UIDB/04050/2020 (CBMA), and UIDB/04469/2020 (CEB), as well as the Research Center of the Portuguese Oncology Institute of Porto (project no. PI86-CI-IPOP-66-2019), and BioTecNorte operation (NORTE-01-0145-FEDER- 000004) funded by the European Regional Development Fund under the scope of Norte 2020 - Programa Operacional Regional do Norte. Marlene Lúcio thanks FCT and ERDF for her doctoral position (CTTI-150/18-CF (1) within the scope of the CONCERT project. Raul Machado acknowledges FCT I.P. for funding within the Scientific Employment Stimulus project (CEECIND/00526/2018).
info:eu-repo/semantics/publishedVersion