Abstract

Resveratrol (RSV) and omega 3 (ω3), 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 ω3 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.

Highlights

  • Dermatological autoimmune diseases [1] are characterized by unbalanced immune responses that contribute to the pathogenesis [2,3]

  • Lipids are found in the interlamellar regions of the stratum corneum and act as a significant barrier to drug permeation [38]

  • The anti-inflammatory effects of lipid nanosystems were evaluated based on their ability to inhibit the cyclooxygenase (COX) activity using a commercial COX Fluorescent

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Summary

Introduction

Dermatological autoimmune diseases (e.g., psoriasis) [1] are characterized by unbalanced immune responses that contribute to the pathogenesis [2,3]. NO is produced in small amounts with an anti-inflammatory effect [7]; in patological conditions, large amounts of NO may be produced, leading to the destruction of skin tissues due to the inflammatory response of the immune cells [8] This type of disease has a major negative impact on patient quality of life due to the characteristics of the symptoms associated with it. Since there is no effective cure for the different types of chronic inflammatory and autoimmune skin conditions, the main purpose of the available therapeutic options is to improve the quality of life of patients by relieving symptoms and slowing the progression of inflammatory conditions This highlights the potential use of inhibitors of NO synthesis and COX activity as an effective modality of treatment in autoimmune and inflammatory skin diseases [5,6,8]

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