Abstract

In the present work, we focused on extracting, separating, formulating, and, finally, characterizing quercetin. Chitosan/GMO nanoparticles were investigated to controlled release for targeting colonic region. Quercetin is an active biomolecule isolated from peels of pomegranate fruit, separated by different chromatographic techniques, and formulated into nanoformulation to bring it to increase its aqueous solubility. Nanoparticles were prepared by using chitosan, glyceryl monooleate (GMO), and poloxamer 407 using probe sonicator and high-pressure homogenization method. Characterization of nanoparticles was carried out by particle size, zeta potential, differential scanning colorimetry (DSC), X-ray diffraction (XRD), scanning electron microscope (SEM), entrapment efficiency, loading content, in vitro release, and stability study. They showed approximately 78.82% encapsulation with an average size of 145.5 ± 0.66 nm and zeta potential + 14.7 mV. The cumulative in vitro drug release up to 24 h at 77.16% was achieved suggesting towards efficacy of green synthesized chitosan nanoparticles for colonic delivery applications. From all our findings, it can be concluded that work will facilitate the extraction, design, and fabrication of nanoparticles for the protection and sustained release of quercetin biomolecule, particularly to the colonic region. The release performance of chitosan/GMO nanoparticles loaded with quercetin at different pH conditions was greatly affected by the materials used in the preparation, which allows maximum release at colonic pH. Hence, it is a unique approach for colonic delivery of drugs having appropriate site specificity and feasibility and controlled release of biomolecule quercetin.

Graphical abstract

Biomolecule quercetin isolated from peels of pomegranate fruit, then separated and characterized by Column, Flash, GC, IR, NMR, LC-MS, HPLC and HPTLC techniques. Formulation and characterization of Qu-loaded Chi nanoparticles by FTIR, XRD, DSC, SEM, Encapsulation effiency and Loading content results influencing on critical quality attributes analysed by central composite design. Optimized Qu-loaded Chi nanoparticles had a significant sustained in-vitrorelease at colonic region.

中文翻译：

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绿色方法合成和表征用于槲皮素体外释放的GMO /壳聚糖纳米颗粒：从石榴果皮中分离

摘要

在当前的工作中，我们专注于提取，分离，配制和最后表征槲皮素。研究了壳聚糖/ GMO纳米颗粒对靶结肠区域的控制释放。槲皮素是一种从石榴果皮中分离出来的活性生物分子，通过不同的色谱技术进行分离，然后配制成纳米制剂以提高其水溶性。通过使用壳聚糖，甘油单油酸酯（GMO）和泊洛沙姆407（使用探针超声仪和高压均质化方法）制备纳米颗粒。纳米粒子的表征是通过粒度，ζ电位，差示扫描比色法（DSC），X射线衍射（XRD），扫描电子显微镜（SEM），包封率，负载量，体外释放和稳定性研究来进行的。他们显示出约78.82％的封装率，平均大小为145.5±0.66 nm，ζ电位+ 14.7 mV。达到了在24小时内达到77.16％的累积体外药物释放，这表明绿色合成的壳聚糖纳米粒子可有效地应用于结肠递送。根据我们所有的发现，可以得出结论，这项工作将促进纳米颗粒的提取，设计和制造，以保护并持续释放槲皮素生物分子，特别是向结肠区域释放。负载槲皮素的壳聚糖/ GMO纳米颗粒在不同pH条件下的释放性能受到制备中所用材料的极大影响，从而在结肠pH值下具有最大释放量。因此，

图形概要

从石榴果皮中分离出生物分子槲皮素，然后通过色谱柱，快速色谱，GC，IR，NMR，LC-MS，HPLC和HPTLC技术进行分离和表征。FTIR，XRD，DSC，SEM，包封效率和负载量的确定和表征Qu负载的Chi纳米颗粒的结果影响了通过中央复合设计分析的关键质量属性。优化的Qu负载Chi纳米颗粒在结肠区域具有显着的持续体外释放。