title: Silymarin-Loaded Nanoparticles Based on Stearic Acid-Modified Bletilla striata Polysaccharide for Hepatic Targeting.
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.
authors.affiliation: Institute of Clinical Pharmacology, General Hospital of Ningxia Medical University, Yinchuan, Ningxia 750004, China. yannima2015@sina.com.
authors.forename: Yanni
authors.initials: Y
authors.lastname: Ma
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Ningxia Medical University, 1160 Shengli Street, Yinchuan, Ningxia 750004, China. 15296907978@163.com.
authors.forename: Shaolong
authors.initials: S
authors.lastname: He
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Ningxia Medical University, 1160 Shengli Street, Yinchuan, Ningxia 750004, China. xueqinma2015@126.com.
authors.forename: Xueqin
authors.initials: X
authors.lastname: Ma
authors.affiliation: Department of Pharmacy, General Hospital of Yankuang Group, Zou Cheng, Shandong 273500, China. tongtonghong2015@sina.com.
authors.forename: Tongtong
authors.initials: T
authors.lastname: Hong
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Ningxia Medical University, 1160 Shengli Street, Yinchuan, Ningxia 750004, China. lizhifang2015@sina.com.
authors.forename: Zhifang
authors.initials: Z
authors.lastname: Li
authors.affiliation: Departments of Biomedical Engineering and Pharmaceutics, Purdue University, West Lafayette, IN 47907, USA. kpark@purdue.edu.
authors.forename: Kinam
authors.initials: K
authors.lastname: Park
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Ningxia Medical University, 1160 Shengli Street, Yinchuan, Ningxia 750004, China. wpwang2015@126.com.
authors.forename: Wenping
authors.initials: W
authors.lastname: Wang
mesh_terms: D061605:Administration, Intravenous; D000818:Animals; D001682:Biological Availability; D002470:Cell Survival / Q000187:drug effects; D004339:Drug Compounding; D016503:Drug Delivery Systems / Q000379:methods*; D065546:Drug Liberation; D006001:Glycoconjugates / Q000138:chemical synthesis; D056945:Hep G2 Cells; D006801:Humans; D007700:Kinetics; D008099:Liver / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D008823:Micelles; D053758:Nanoparticles / Q000737:chemistry* / Q000378:metabolism / Q000648:ultrastructure; D029595:Orchidaceae / Q000737:chemistry*; D011134:Polysaccharides / Q000737:chemistry* / Q000302:isolation & purification; D012838:Silymarin / Q000737:chemistry / Q000493:pharmacokinetics*; D013229:Stearic Acids / Q000737:chemistry*
chemical_list: D006001:Glycoconjugates; D008823:Micelles; D011134:Polysaccharides; D012838:Silymarin; D013229:Stearic Acids; C000591471:polysaccharide b, Bletilla striata; C031183:stearic acid
keywords: Bletilla striata; hepatic targeting; nanoparticles; polysaccharide; silymarin