Curcumin and Quercetin-Loaded Lipid Nanocarriers: Development of Omega-3 Mucoadhesive Nanoemulsions for Intranasal Administration. 2022

Gustavo Richter Vaz, and Mariana Corrêa Falkembach Carrasco, and Matheus Monteiro Batista, and Paula Alice Bezerra Barros, and Meliza da Conceição Oliveira, and Ana Luiza Muccillo-Baisch, and Virginia Campello Yurgel, and Francesca Buttini, and Félix Alexandre Antunes Soares, and Larissa Marafiga Cordeiro, and Flavia Fachel, and Helder Ferreira Teixeira, and Juliana Bidone, and Patrícia Diaz de Oliveira, and Fabio Sonvico, and Cristiana Lima Dora
Graduate Program in Health Sciences, Federal University of Rio Grande, Rio Grande 96203-900, Brazil.

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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