Trans-resveratrol-loaded nonionic lamellar liquid-crystalline systems: structural, rheological, mechanical, textural, and bioadhesive characterization and evaluation of in vivo anti-inflammatory activity

• Published in: International journal of nanomedicine Vol. 12; pp. 6883 - 6893
• Main Authors: Fonseca-Santos, Bruno, Satake, Cínthia Yuka, Calixto, Giovana Maria Fioramonti, Dos Santos, Aline Martins, Chorilli, Marlus
• Format: Journal Article
• Language: English
• Published: New Zealand Dove Medical Press Limited 01.01.2017; Taylor & Francis Ltd; Dove Medical Press
• Subjects: Adhesiveness; Adhesives - pharmacology; Animals; Anti-Inflammatory Agents - chemistry; Anti-Inflammatory Agents - pharmacology; anti-inflammatory properties; Castor oil; Dosage and administration; Drug delivery systems; Health aspects; Humans; Hydrogenation; Ions; lamellar mesophase; Lipids; liquid crystals; Liquid Crystals - chemistry; Male; Materials Testing; Mechanical Phenomena; Mice; Microscopy; Original Research; Peanuts; Phase transitions; Polyethylene glycol; Resveratrol; Rheology; Scattering, Small Angle; Skin - drug effects; Skin diseases; Solubility; Stilbenes - chemistry; Stilbenes - pharmacology; Surfactants; Sus scrofa; topical delivery; Transdermal medication; Wine; X-Ray Diffraction; Brazil; United States > US; topical delivery; lamellar mesophase; liquid crystals; anti-inflammatory properties
• ISSN: 1178-2013; 1176-9114; 1178-2013
• DOI: 10.2147/IJN.S138629

Resveratrol (Res) is a common phytoalexin present in a few edible materials, such as grape skin, peanuts, and red wine. Evidence has shown the beneficial effects of Res on human health, which may be attributed to its anti-inflammatory activity. However, the poor aqueous solubility of Res limits its therapeutic effectiveness. Therefore, the use of nanostructured delivery systems for Res, such as liquid-crystalline systems, could be beneficial. In this study, we aimed to develop, characterize, and determine the in vivo effectiveness of Res-loaded liquid-crystalline systems. Systems containing copaiba balsam oil, polyethylene glycol-40 hydrogenated castor oil, and water were designed. Results of polarized light microscopy, small-angle X-ray scattering, texture-profile analysis, and flow-rheology analysis showed that the Res-loaded liquid-crystalline system had a lamellar structure, textural and mechanical (hardness, compressibility, and adhesiveness) properties, and behaved as a non-Newtonian fluid, showing pseudoplastic behavior upon skin application. Furthermore, all liquid-crystalline systems presented bioadhesive properties that may have assisted in maintaining the anti-inflammatory activity of Res, since the topical application of the Res-loaded lamellar mesophase liquid crystals resulted in edema inhibition in a carrageenan-induced paw-inflammation mouse model. Therefore, Res-loaded lamellar mesophases represent a promising new therapeutic approach for inhibition of skin inflammation.