4.7 Article

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

Journal

INTERNATIONAL JOURNAL OF NANOMEDICINE
Volume 12, Issue -, Pages 6883-6893

Publisher

DOVE MEDICAL PRESS LTD
DOI: 10.2147/IJN.S138629

Keywords

lamellar mesophase; liquid crystals; anti-inflammatory properties; topical delivery

Funding

  1. National Council of Technological and Scientific Development (CNPq)
  2. Sao Paulo Research Foundation (FAPESP) [14/24180-0]
  3. Programa de Apoio ao Desenvolvimento Cientifico (PADC)
  4. Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [14/24180-0] Funding Source: FAPESP

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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.

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