Formulation and modification of physicochemical parameters of p-Coumaric acid by cyclodextrin nanosponges

IF 1.7 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY
Anil Kumar, Rekha Rao
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引用次数: 5

Abstract

Reactive oxygen species triggered oxidative stress contributes to the pathogenesis of numerous ailments such as myocardial infraction, inflammation, atherosclerosis, and pigmentation disorders. ROS scavengers, particularly natural bioactives are one of the possible options to reduce this stress. However, these bioactives possess certain formulation challenges owing to their poor solubility, stability, and bioavailability. Therefore, the design of a stable formulation that can deal these challenges, while preserving the antioxidant efficacy is of great significance. In this view, the current study was aimed at fabrication of p-Coumaric acid loaded nanosponges employing melt method. The spectroscopy resulting nanosponges were appropriately characterized using Fourier transform infrared spectroscopy, X-ray powder diffraction, differential scanning calorimetry, thermogravimetric analysis, nuclear magnetic resonance, FE-SEM (field emission scanning electron microscopy) and TEM (transmission electron microscopy). The particle size of PCA-CDNS (p-Coumaric acid nanosponges) was in nano range, with low PDI (polydispersity index), acceptable zeta potential and delayed release. Molecular docking studies for PCA using mushroom tyrosinase (TYR) were also carried out. Further, the antioxidant and antityrosinase studies were also performed. In nutshell, the findings herein revealed that encasement of PCA in NS led to an enhancement in efficacy of this bioactive in terms of safety, solubility, and release, while preserving its antioxidant and antityrosinase effects. On the basis of the present results, we expect that PCA nanosponges can be seen as promising carriers for addressing depigmention, particularly associated with ROS overexpression.

Abstract Image

环糊精纳米海绵制备对香豆酸及其理化参数的修饰
活性氧引发的氧化应激有助于许多疾病的发病机制,如心肌梗死、炎症、动脉粥样硬化和色素沉着障碍。活性氧清除剂,特别是天然生物活性物质是减少这种压力的可能选择之一。然而,由于其溶解度、稳定性和生物利用度差,这些生物活性物质具有一定的配方挑战。因此,设计一种稳定的配方,既能应对这些挑战,又能保持其抗氧化功效具有重要意义。因此,本研究旨在利用熔融法制备对香豆酸负载的纳米海绵。利用傅里叶变换红外光谱、x射线粉末衍射、差示扫描量热法、热重分析、核磁共振、场发射扫描电镜(FE-SEM)和透射电镜(TEM)对所得纳米海绵进行了表征。PCA-CDNS(对香豆酸纳米海绵)粒径在纳米范围内,具有较低的PDI(多分散性指数),良好的zeta电位和缓释。利用蘑菇酪氨酸酶(TYR)对PCA进行了分子对接研究。此外,还进行了抗氧化和抗酪氨酸酶的研究。简而言之,本文的研究结果表明,在NS中包裹PCA导致该生物活性在安全性,溶解度和释放方面的功效增强,同时保持其抗氧化和抗酪氨酸酶的作用。基于目前的结果,我们期望PCA纳米海绵可以被视为解决色素褪色的有希望的载体,特别是与ROS过表达相关的载体。
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来源期刊
Journal of Inclusion Phenomena and Macrocyclic Chemistry
Journal of Inclusion Phenomena and Macrocyclic Chemistry Agricultural and Biological Sciences-Food Science
CiteScore
4.10
自引率
8.70%
发文量
54
期刊介绍: The Journal of Inclusion Phenomena and Macrocyclic Chemistry is the premier interdisciplinary publication reporting on original research into all aspects of host-guest systems. Examples of specific areas of interest are: the preparation and characterization of new hosts and new host-guest systems, especially those involving macrocyclic ligands; crystallographic, spectroscopic, thermodynamic and theoretical studies; applications in chromatography and inclusion polymerization; enzyme modelling; molecular recognition and catalysis by inclusion compounds; intercalates in biological and non-biological systems, cyclodextrin complexes and their applications in the agriculture, flavoring, food and pharmaceutical industries; synthesis, characterization and applications of zeolites. The journal publishes primarily reports of original research and preliminary communications, provided the latter represent a significant advance in the understanding of inclusion science. Critical reviews dealing with recent advances in the field are a periodic feature of the journal.
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