Preparation of chitosan-coated hollow tin dioxide nanoparticles and their application in improving the oral bioavailability of febuxostat

IF 5.2 2区 医学 Q1 PHARMACOLOGY & PHARMACY International Journal of Pharmaceutics: X Pub Date : 2023-07-13 DOI:10.1016/j.ijpx.2023.100199
Junpeng Sun , Jiaqun Du , Xiaobang Liu , Jinyu An , Yingqiao Li , Yanan Yu , Minghui Li , Li Zheng , Chao Wu , Lili Hu
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引用次数: 2

Abstract

The aim of this study was to design a chitosan-coated hollow tin dioxide nanosphere (CS-HSn) for loading febuxostat (FEB) using an adsorption method to obtain a sustained-release system (CS-HSn-FEB) to improve the oral bioavailability of FEB. The morphological characteristics of hollow tin dioxide nanospheres (HSn) and CS-HSn were analyzed by transmission electron microscopy (TEM) and dynamic light scattering (DLS). The hemolysis test and CCK-8 test were used to assess the biosafety of HSn and CS-HSn. Powder X-ray diffraction (PXRD) and differential scanning thermal analysis (DSC) were performed on CS-HSn-FEB to analyze the drug presence status. The dissolution behavior and changes in plasma drug concentration of CS-HSn-FEB were evaluated in vitro and in vivo. Sections of intestinal tissues from SD rats were obtained to observe whether chitosan could increase the distribution of nanoparticles in the intestinal tissues. The results showed that FEB was present in CS-HSn in an amorphous state. Moreover, CS-HSn, with good biosafety, significantly improved the water solubility and oral absorption of FEB, indicating that CS-HSn has great potential to improve the intestinal absorption and oral bioavailability of insoluble drugs.

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壳聚糖包被中空二氧化锡纳米颗粒的制备及其在提高非布司他口服生物利用度中的应用
本研究的目的是设计一种壳聚糖包覆的中空二氧化锡纳米球(CS-HSn),用吸附法负载非布司他(FEB),获得一种缓释系统(CS-HSn-FEB),以提高FEB的口服生物利用度。通过透射电子显微镜(TEM)和动态光散射(DLS)分析了中空二氧化锡纳米球(HSn)和CS HSn的形态特征。采用溶血试验和CCK-8试验评价HSn和CS HSn的生物安全性。对CS-HSn-FEB进行了粉末X射线衍射(PXRD)和差示扫描热分析(DSC),分析了药物的存在状态。在体外和体内评价了CS HSn FEB的溶出行为和血浆药物浓度的变化。取SD大鼠肠组织切片,观察壳聚糖是否能增加纳米颗粒在肠组织中的分布。结果表明,FEB以非晶态存在于CS-HSn中。此外,具有良好生物安全性的CS HSn显著提高了FEB的水溶性和口服吸收,表明CS HSn在提高不溶性药物的肠道吸收和口服生物利用度方面具有巨大潜力。
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来源期刊
International Journal of Pharmaceutics: X
International Journal of Pharmaceutics: X Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
6.60
自引率
0.00%
发文量
32
审稿时长
24 days
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