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Molecules 2016, 21(3), 265; doi:10.3390/molecules21030265

Silymarin-Loaded Nanoparticles Based on Stearic Acid-Modified Bletilla striata Polysaccharide for Hepatic Targeting

1
Institute of Clinical Pharmacology, General Hospital of Ningxia Medical University, Yinchuan, Ningxia 750004, China
2
Department of Pharmaceutics, School of Pharmacy, Ningxia Medical University, 1160 Shengli Street, Yinchuan, Ningxia 750004, China
3
Department of Pharmacy, General Hospital of Yankuang Group, Zou Cheng, Shandong 273500, China
4
Departments of Biomedical Engineering and Pharmaceutics, Purdue University, West Lafayette, IN 47907, USA
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 18 January 2016 / Revised: 15 February 2016 / Accepted: 22 February 2016 / Published: 29 February 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [2724 KB, uploaded 29 February 2016]   |  

Abstract

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. View Full-Text
Keywords: silymarin; Bletilla striata; polysaccharide; nanoparticles; hepatic targeting silymarin; Bletilla striata; polysaccharide; nanoparticles; hepatic targeting
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Ma, Y.; He, S.; Ma, X.; Hong, T.; Li, Z.; Park, K.; Wang, W. Silymarin-Loaded Nanoparticles Based on Stearic Acid-Modified Bletilla striata Polysaccharide for Hepatic Targeting. Molecules 2016, 21, 265.

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