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负载人参皂苷Rb的pH敏感型壳聚糖-脱氧胆酸-海藻酸钠纳米粒的制备及其控释机制

Preparation of pH-sensitive chitosan-deoxycholic acid-sodium alginate nanoparticles loaded with ginsenoside Rb and its controlled release mechanism.

作者信息

Dong Yujia, He Yanhui, Fan Daidi, Wu Zhansheng

机构信息

School of Environmental and Chemical Engineering, Xi'an Key Laboratory of Textile Chemical Engineering Auxiliaries, Xi'an Polytechnic University, Xi'an 710048, PR China.

School of Environmental and Chemical Engineering, Xi'an Key Laboratory of Textile Chemical Engineering Auxiliaries, Xi'an Polytechnic University, Xi'an 710048, PR China.

出版信息

Int J Biol Macromol. 2023 Apr 15;234:123736. doi: 10.1016/j.ijbiomac.2023.123736. Epub 2023 Feb 16.

Abstract

Ginsenoside is a natural extract of the genus ginseng, which has tumor preventive and inhibiting effects. In this study, ginsenoside loaded nanoparticles were prepared by an ionic cross-linking method with sodium alginate to enable a sustained slow release effect of ginsenoside Rb in the intestinal fluid through an intelligent response. Chitosan grafted hydrophobic group deoxycholic acid was used to synthesize CS-DA, providing loading space for hydrophobic Rb. Scanning electron microscopy (SEM) showed that the nanoparticles was spherical with smooth surfaces. The encapsulation rate of Rb enhanced with the increase of sodium alginate concentration and could reach to 76.62 ± 1.78 % when concentration was 3.6 mg/mL. It was found that the release process of CDA-NPs was most consistent with the primary kinetic model which is a diffusion-controlled release mechanism. CDA-NPs exhibited good pH sensitivity and controlled release properties in buffer solutions of different pH's at 1.2 and 6.8. The cumulative release of Rbfrom CDA-NPs in simulated gastric fluid was <20 % within 2 h, while could release completely around 24 h in the simulated gastrointestinal fluid release system. It was demonstrated that CDA-NPs can effectively control release and intelligently deliver ginsenoside Rb, which is a promising alternative way for oral delivery.

摘要

人参皂苷是人参属的一种天然提取物,具有肿瘤预防和抑制作用。在本研究中,采用离子交联法与海藻酸钠制备了负载人参皂苷的纳米颗粒,通过智能响应使人参皂苷Rb在肠液中实现持续缓慢释放效果。使用接枝了疏水基团脱氧胆酸的壳聚糖合成CS-DA,为疏水性的Rb提供负载空间。扫描电子显微镜(SEM)显示纳米颗粒呈球形,表面光滑。Rb的包封率随海藻酸钠浓度的增加而提高,当浓度为3.6mg/mL时可达76.62±1.78%。发现CDA-NPs的释放过程最符合一级动力学模型,这是一种扩散控制释放机制。CDA-NPs在pH为1.2和6.8的不同pH缓冲溶液中表现出良好的pH敏感性和控释性能。在模拟胃液中,CDA-NPs中Rb的累积释放率在2小时内<20%,而在模拟胃肠液释放系统中约24小时可完全释放。结果表明,CDA-NPs能够有效控制释放并智能递送人参皂苷Rb,这是一种有前景的口服给药替代方式。

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