Preparation, characterization and properties of quercetin cyclodextrin nanosponges

IF 1.6 4区化学 Q2 Agricultural and Biological Sciences Journal of Inclusion Phenomena and Macrocyclic Chemistry Pub Date : 2024-10-22 DOI:10.1007/s10847-024-01263-z

Wanping Zhang, Houchen Gai, Qianjie Zhang, Dongmei Zhang, Shilian Zheng, Guangyong Zhu

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Abstract

Quercetin (QC) has various biological activities such as anti-inflammatory and antibacterial properties. However, due to its poor solubility and stability, the application of QC in clinical practice is limited. Nanosponge (NS), as a new drug carrier, can significantly improve the solubility of low-soluble drug components, and significantly improve the efficacy and bioavailability of drugs. In this paper, cyclodextrin nanosponges (CDNS) were synthesized by cross-linking β-cyclodextrin with diphenyl carbonate (DPC) in a green and safe synthetic pathway. As wall material, CDNS were further used to encapsulate quercetin and quercetin-cyclodextrin nanosponges (QCNS) were formed. The resultant CDNS and QCNS were characterized by scanning electron microscopy, infrared spectroscopy, X-ray diffraction, and thermogravimetric analysis. The results showed that CDNS and QCNS were successful prepared. The solubilizing impact of CDNS on quercetin was investigated. The results showed that its solubility in water was 176 times higher than that of pure QC. The cumulative release of quercetin and QCNS over 48 h and the cumulative transdermal penetration over 12 h were measured. The antioxidant and antibacterial properties of QCNS were determined. QCNS exhibited superior stability, permeability, and sustained-release properties compared to pure quercetin, and had notable bacteriostatic and antioxidant capabilities.

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槲皮素环糊精纳米海绵的制备、表征及性能研究

槲皮素（QC）具有抗炎、抗菌等多种生物活性。但由于其溶解度和稳定性较差，限制了QC在临床中的应用。纳米海绵（Nanosponge， NS）作为一种新型药物载体，可以显著提高低溶性药物成分的溶解度，显著提高药物的药效和生物利用度。采用绿色安全的合成途径，利用β-环糊精与碳酸二苯酯交联制备了环糊精纳米海绵（CDNS）。进一步以槲皮素为壁材包封槲皮素，形成槲皮素-环糊精纳米海绵。用扫描电镜、红外光谱、x射线衍射和热重分析对合成的CDNS和QCNS进行了表征。结果表明，CDNS和QCNS均制备成功。研究了CDNS对槲皮素的增溶作用。结果表明，其在水中的溶解度是纯QC的176倍。测定槲皮素和QCNS在48 h内的累积释放量和12 h内的累积透皮渗透量。测定了QCNS的抗氧化和抗菌性能。与纯槲皮素相比，QCNS具有更好的稳定性、渗透性和缓释性能，并具有显著的抑菌和抗氧化能力。

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来源期刊

Journal of Inclusion Phenomena and Macrocyclic Chemistry 化学-化学综合

CiteScore

3.30

自引率

8.70%

发文量

审稿时长

3-8 weeks

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.