Vaz Gustavo Richter, Carrasco Mariana Corrêa Falkembach, Batista Matheus Monteiro, Barros Paula Alice Bezerra, Oliveira Meliza da Conceição, Muccillo-Baisch Ana Luiza, Yurgel Virginia Campello, Buttini Francesca, Soares Félix Alexandre Antunes, Cordeiro Larissa Marafiga, Fachel Flavia, Teixeira Helder Ferreira, Bidone Juliana, de Oliveira Patrícia Diaz, Sonvico Fabio, Dora Cristiana Lima
Graduate Program in Health Sciences, Federal University of Rio Grande, Rio Grande 96203-900, Brazil.
Food and Drug Department, University of Parma, 43124 Parma, Italy.
Nanomaterials (Basel). 2022 Mar 25;12(7):1073. doi: 10.3390/nano12071073.
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 . 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.
姜黄素（CUR）和槲皮素（QU）因其抗炎和抗氧化特性，是治疗诸如神经退行性疾病（ND）等脑部疾病的潜在化合物。然而，低水溶性和差的生物利用度阻碍了它们的临床应用。在此背景下，纳米技术作为一种克服生物制药问题的策略应运而生。在这项工作中，我们开发、表征、比较并优化了三种不同的负载CUR和QU的ω-3（ω-3）脂肪酸纳米乳剂（NEs）（阴性、阳离子、凝胶型），它们通过两种不同方法制备，用于鼻内给药（IN）。结果表明，用两种提议方法制备的制剂表现出良好的稳定性，并且能够包载相似量的CUR和QU。另一方面，观察到粒径、ζ电位、体外释放动力学以及渗透/滞留试验存在差异。考虑到所测试的两种制备方法，高压均质法（HPH）显示出优势，并且所得到的CQ NE-表现出缓释潜力。毒性研究表明这些制剂对……无毒。所开发的ω-3脂肪酸NEs对于脑部疾病的治疗已显示出一系列有趣的特性，因为它们有潜力增加CUR和QU的鼻脑渗透，从而提高治疗效率。
