Silymarin-Loaded Nanoparticles Based on Stearic Acid-Modified Bletilla striata Polysaccharide for Hepatic Targeting.
Silymarin-Loaded Nanoparticles Based on Stearic Acid-Modified Bletilla striata Polysaccharide for Hepatic Targeting.
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DOI：
10.3390/molecules21030265
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发表时间：
2016-02-29
期刊：
影响因子：
--
通讯作者：
Wang W
中科院分区：
文献类型：
--
作者：
Ma Y;He S;Ma X;Hong T;Li Z;Park K;Wang W
水飞蓟素作为一种保肝药物已广泛用于多种肝脏疾病的治疗，然而其口服后的有效性因水溶性差和生物利用度低而受到影响，因此有必要开发静脉注射产品，尤其是用于肝靶向的产品。在本研究中，水飞蓟素被包封在经硬脂酸修饰的白及多糖（BSP）共轭物自组装纳米粒中，并对所得纳米粒的理化性质进行了表征。在透射电子显微镜下，载有水飞蓟素的胶束呈球形颗粒，平均直径为200纳米。通过差示扫描量热分析图和X射线衍射图分别证实了药物分子的包封。这些纳米粒呈现出近1周的缓释特性，且无明显的初始突释现象。与药物溶液相比，载药纳米粒在HepG2细胞系上表现出较低的细胞活力和较高的摄取强度。给小鼠静脉注射纳米粒制剂30分钟后，肝脏成为富集荧光探针最显著的器官。这些结果表明，BSP衍生纳米粒具有肝靶向能力，是将水飞蓟素递送至肝脏的有前景的纳米载体。
Silymarin has been widely used as a hepatoprotective drug in the treatment of various liver diseases, yet its effectiveness is affected by its poor water solubility and low bioavailability after oral administration, and there is a need for the development of intravenous products, especially for liver-targeting purposes. In this study, silymarin was encapsulated in self-assembled nanoparticles of Bletilla striata polysaccharide (BSP) conjugates modified with stearic acid and the physicochemical properties of the obtained nanoparticles were characterized. The silymarin-loaded micelles appeared as spherical particles with a mean diameter of 200 nm under TEM. The encapsulation of drug molecules was confirmed by DSC thermograms and XRD diffractograms, respectively. The nanoparticles exhibited a sustained-release profile for nearly 1 week with no obvious initial burst. Compared to drug solutions, the drug-loaded nanoparticles showed a lower viability and higher uptake intensity on HepG2 cell lines. After intravenous administration of nanoparticle formulation for 30 min to mice, the liver became the most significant organ enriched with the fluorescent probe. These results suggest that BSP derivative nanoparticles possess hepatic targeting capability and are promising nanocarriers for delivering silymarin to the liver.
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