Institute of Clinical Pharmacology, General Hospital of Ningxia Medical University, Yinchuan, Ningxia 750004, China.
Department of Pharmaceutics, School of Pharmacy, Ningxia Medical University, 1160 Shengli Street, Yinchuan, Ningxia 750004, China.
Molecules. 2016 Feb 29;21(3):265. doi: 10.3390/molecules21030265.
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.
水飞蓟素被广泛用作治疗各种肝脏疾病的保肝药物，但由于其水溶性差和口服后生物利用度低，需要开发静脉产品，特别是用于肝脏靶向的产品。在这项研究中，水飞蓟素被包封在经过硬脂酸修饰的白芨多糖（BSP）缀合物自组装纳米粒子中，并且对所得到的纳米粒子的物理化学性质进行了表征。TEM 下显示载药水飞蓟素胶束为球形颗粒，平均直径为 200nm。通过 DSC 热谱图和 XRD 衍射图分别证实了药物分子的包封。纳米粒子表现出近 1 周的持续释放曲线，没有明显的初始突释。与药物溶液相比，载药水飞蓟素纳米粒子在 HepG2 细胞系中表现出较低的细胞活力和更高的摄取强度。将纳米粒制剂静脉注射到小鼠体内 30 分钟后，肝脏成为富含荧光探针的最重要器官。这些结果表明，BSP 衍生物纳米粒子具有肝靶向能力，是将水飞蓟素递送到肝脏的有前途的纳米载体。
