Evaluation of stability and anxiolytic potential of oil-in-water polysaccharide nanoemulsions loaded with chalcone (1E,4E)-1,5-bis(4-methoxyphenyl) penta-1,4-dien-3-one

IF 2.2 4区 化学 Q2 Engineering
Joice Farias do Nascimento, Flavia Oliveira Monteiro da Silva Abreu, Taysse Holanda, Rachel Menezes Castelo, Helcio Silva dos Santos, Jane Eire Silva Alencar de Menezes, Jesyka Macêdo Guedes
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Abstract

The desire for products that are healthier, safer, and better for the environment is on the rise in society. Chalcones are aromatic ketones with anxiolytic and antimicrobial properties. The limited solubility, bioavailability, and long-term stability of chalcones hinder their application. Nanoemulsions can be used as a drug transport system to address this problem. The primary objective of our research was to design nanoemulsions through ANOVA (NE) with nanoscale droplets that would maintain exceptional stability, optimizing the anxiolytic capacity of chalcones. Sodium alginate and chitosan were assessed as the continuous phase material, while commercial soybean oil and mineral oil were used as adjuvants, besides surfactant, for the oil phase composition of the droplets. Results showed that the addition of soybean oil improved significantly the stability of the formulations, as did the use of the alginate matrix. The optimal NE showed a nanometer-sized droplet (126 nm) and negative ζ-potential (− 42 mV), showing good stability under different conditions—it synergistically enhances the anxiolytic potential. The mode of operation is associated with the receptors of the serotonergic system (5-HT). Toxicity, locomotion and anxiety tests performed using the zebrafish animal model showed a promising dose (0.0325 mg/mL) for the development of compounds with anxiolytic properties.

Graphical abstract

Abstract Image

评估水包油多糖纳米乳液负载查尔酮 (1E,4E)-1,5-双(4-甲氧基苯基)五-1,4-二烯-3-酮的稳定性和抗焦虑潜力
社会对更健康、更安全、更环保的产品的需求日益增长。查耳酮是一种芳香酮,具有抗焦虑和抗菌特性。查耳酮的溶解度、生物利用度和长期稳定性有限,阻碍了其应用。纳米乳剂可作为药物运输系统来解决这一问题。我们研究的主要目的是通过方差分析(NE)设计纳米级液滴的纳米乳剂,使其保持优异的稳定性,优化查耳酮的抗焦虑能力。海藻酸钠和壳聚糖被评估为连续相材料,而商用大豆油和矿物油则被用作除表面活性剂外的辅助剂,用于液滴的油相组成。结果表明,添加大豆油能显著提高配方的稳定性,使用海藻酸基质也是如此。最佳 NE 显示出纳米级大小的液滴(126 nm)和负ζ电位(- 42 mV),显示出在不同条件下的良好稳定性--它协同增强了抗焦虑潜能。其工作模式与血清素能系统(5-HT)受体有关。利用斑马鱼动物模型进行的毒性、运动和焦虑测试表明,该剂量(0.0325 毫克/毫升)有望用于开发具有抗焦虑特性的化合物。
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来源期刊
Chemical Papers
Chemical Papers Chemical Engineering-General Chemical Engineering
CiteScore
3.30
自引率
4.50%
发文量
590
期刊介绍: Chemical Papers is a peer-reviewed, international journal devoted to basic and applied chemical research. It has a broad scope covering the chemical sciences, but favors interdisciplinary research and studies that bring chemistry together with other disciplines.
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