A New Type of Liquid Silymarin Proliposome Containing Bile Salts: Its Preparation and Improved Hepatoprotective Effects

被引:15
作者
Wang, Mei [1 ]
Xie, Tingting [2 ]
Chang, Zhanying [1 ]
Wang, Ling [1 ]
Xie, Xiangyun [1 ]
Kou, Yaohong [1 ]
Xu, Hongxia [1 ]
Gao, Xiaoli [1 ]
机构
[1] Xinjiang Med Univ, Coll Pharm, Dept Pharmaceut, Urumqi, Peoples R China
[2] Peoples Liberat Army Gen Hosp, Dept Pharmaceut Care, Beijing, Peoples R China
来源
PLOS ONE | 2015年 / 10卷 / 12期
关键词
IMPROVED ORAL DELIVERY; IN-VITRO EVALUATION; LIPOSOMES; BIOAVAILABILITY; SYSTEM; FORMULATION; LIPIDS; MODEL;
D O I
10.1371/journal.pone.0143625
中图分类号
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号
07 ; 0710 ; 09 ;
摘要
Silymarin, a known extract, is used in the treatment of liver diseases with various origins, but its current administration form cannot target the liver because of its poor oral bioavailability. A new type of oral silymarin proliposome aimed at improving silymarin's poor bioavailability and hepatoprotective effects, is introduced in this work. Silymarin-loaded liquid proliposome were prepared using a simple dissolving process. The morphology, particle size, zeta potential, and entrapment efficiency of the silymarin liposomes were analysed. The everted gut sac transport model was used to measure the intestinal transport of liposomes. The liposomal hepatoprotective activity was evaluated in three types of experimental hepatitis animal models. After staining with haematoxylin and eosin, the livers were microscopically examined to analyse any pathological changes. The prepared silymarin proliposome formed silymarin liposomes with a multilayer liposome structure and improved intestinal transport. In an injured liver, the silymarin liposomes produced a stronger hepatoprotective effect through a significant decrease in both the aminotransferase and MDA levels and a significant increase in the SOD and GSH-PX levels compared to orally administered silymarin tablets. This effect was also confirmed histopathologically. In a word, incorporation of silymarin into a liposomal carrier system increased intestinal absorption and showed better hepatoprotective effects compared to silymarin tablets.
引用
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页数:15
相关论文
共 31 条
[1]   Everted gut sac model as a tool in pharmaceutical research: limitations and applications [J].
Alam, Mohd Aftab ;
Al-Jenoobi, Fahad Ibrahim ;
Al-mohizea, Abdullah M. .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 2012, 64 (03) :326-336
[2]   PHARMACOKINETIC STUDIES ON IDB-1016, A SILYBIN-PHOSPHATIDYLCHOLINE COMPLEX, IN HEALTHY-HUMAN SUBJECTS [J].
BARZAGHI, N ;
CREMA, F ;
GATTI, G ;
PIFFERI, G ;
PERUCCA, E .
EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS, 1990, 15 (04) :333-338
[3]   Oral bioavailability of silymarin formulated as a novel 3-day delivery system based on porous silica nanoparticles [J].
Cao, Xia ;
Fu, Min ;
Wang, Liang ;
Liu, Hongfei ;
Deng, Wenwen ;
Qu, Rui ;
Su, Weiyan ;
Wei, Yawei ;
Xu, Ximing ;
Yu, Jiangnan .
ACTA BIOMATERIALIA, 2012, 8 (06) :2104-2112
[4]   Enhanced bioavailability of the poorly water-soluble drug fenofibrate by using liposomes containing a bile salt [J].
Chen, Yaping ;
Lu, Yi ;
Chen, Jianming ;
Lai, Jie ;
Sun, Jing ;
Hu, Fuqiang ;
Wu, Wei .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2009, 376 (1-2) :153-160
[5]   Proliposomes for oral delivery of dehydrosilymarin: preparation and evaluation in vitro and in vivo [J].
Chu, Chang ;
Tong, Shan-shan ;
Xu, Ying ;
Wang, Li ;
Fu, Min ;
Ge, Yan-ru ;
Yu, Jiang-nan ;
Xu, Xi-ming .
ACTA PHARMACOLOGICA SINICA, 2011, 32 (07) :973-980
[6]   Evaluation of hybrid liposomes-encapsulated silymarin regarding physical stability and in vivo performance [J].
El-Samaligy, Mohamed S. ;
Afifi, Nagia N. ;
Mahmoud, Enas A. .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2006, 319 (1-2) :121-129
[7]   Silymarin loaded liposomes for hepatic targeting: In vitro evaluation and HepG2 drug uptake [J].
Elmowafy, Mohammed ;
Viitala, Tapani ;
Ibrahim, Hany M. ;
Abu-Elyazid, Sherif K. ;
Samy, Ahmed ;
Kassem, Alaa ;
Yliperttula, Marjo .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2013, 50 (02) :161-171
[8]  
Gao Xiao-li, 2005, Yaoxue Xuebao, V40, P1139
[9]  
Ghosh A, 2012, J PHARM SCI TECHNOL, V2, P348
[10]   Temperature dependence of the interaction of cholate and deoxycholate with fluid model membranes and their solubilization into mixed micelles [J].
Hildebrand, A ;
Beyer, K ;
Neubert, R ;
Garidel, P ;
Blume, A .
COLLOIDS AND SURFACES B-BIOINTERFACES, 2003, 32 (04) :335-351