Curcumin and Quercetin-Loaded Lipid Nanocarriers: Development of Omega-3 Mucoadhesive Nanoemulsions for Intranasal Administration

载有姜黄素和槲皮素的脂质纳米载体:用于鼻腔给药的 Omega-3 粘膜粘附纳米乳剂的开发

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作者:Gustavo Richter Vaz, Mariana Corrêa Falkembach Carrasco, Matheus Monteiro Batista, Paula Alice Bezerra Barros, Meliza da Conceição Oliveira, Ana Luiza Muccillo-Baisch, Virginia Campello Yurgel, Francesca Buttini, Félix Alexandre Antunes Soares, Larissa Marafiga Cordeiro, Flavia Fachel, Helder Ferrei

Abstract

Curcumin (CUR) and quercetin (QU) are potential compounds for treatment of brain diseases such as neurodegenerative diseases (ND) because of their anti-inflammatory and antioxidant properties. However, low water solubility and poor bioavailability hinder their clinical use. In this context, nanotechnology arises as a strategy to overcome biopharmaceutical issues. In this work, we develop, characterize, compare, and optimize three different omega-3 (ω-3) fatty acids nanoemulsions (NEs) loaded with CUR and QU (negative, cationic, gelling) prepared by two different methods for administration by intranasal route (IN). The results showed that formulations prepared with the two proposed methods exhibited good stability and were able to incorporate a similar amount of CUR and QU. On the other side, differences in size, zeta potential, in vitro release kinetics, and permeation/retention test were observed. Considering the two preparation methods tested, high-pressure homogenization (HPH) shows advantages, and the CQ NE- obtained demonstrated potential for sustained release. Toxicity studies demonstrated that the formulations were not toxic for Caenorhabditis elegans. The developed ω-3 fatty acid NEs have shown a range of interesting properties for the treatment of brain diseases, since they have the potential to increase the nose-to-brain permeation of CUR and QU, enabling enhanced treatments efficiency.

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