水飞蓟宾固体脂质纳米粒的制备及抗肝纤维化作用  

Preparation and anti-fibrotic effects of solid lipid nanoparticles loaded with silibinin

作　　者：厉英超[1] 董蕾[2] 贾皑[1] 苌新明[1] 薛挥[1] 

机构地区：[1]西安交通大学医学院第一附属医院消化内科,陕西西安710061 [2]西安交通大学医学院第二附属医院消化内科,陕西西安710004

出　　处：《西安交通大学学报（医学版）》2007年第5期517-520,共4页Journal of Xi’an Jiaotong University（Medical Sciences）

基　　金：陕西省科技计划资助项目(No.2006K10-G3-2)

摘　　要：目的制备载中药水飞蓟宾(SIL)的固体脂质纳米粒(SLN),并观察其对肝硬化模型大鼠的抗肝纤维化作用。方法采用高压乳匀法制备SIL-SLN,实验大鼠分为正常对照组、模型对照组、SIL普通剂型组、SIL-SLN灌胃组和SIL-SLN静脉注射组,比较SIL的SLN剂型与普通剂型的抗肝纤维化作用。结果高压乳匀法制备的SIL-SLN呈圆形,形态规则,粒径为(157±8)nm,Zeta电位为(-35.36±2.68)mV,平均包封率为95.64%,平均SIL含量为1.501 g/L。给药8周后,SIL-SLN灌胃组和SIL-SLN静脉注射组的大鼠肝脏Masson胶原染色图像分析灰度值分别为4.73±1.35和2.26±0.42,与SIL普通剂型组(7.26±1.72)比较差异有显著性(P<0.05),且SIL-SLN静脉注射组作用优于SIL-SLN灌胃组(P<0.05)。结论SIL-SLN可显著提高SIL的抗肝纤维化作用,静脉注射作用更强,是一种新型中药靶向制剂。Objective To prepare solid lipid nanoparticles （SLN） loaded with silibinin （SIL） extracted from traditional Chinese medicine and study the anti-fibrotic effects in model rats of liver cirrhosis. Methods SIL-SLN was prepared by high pressure homogenization. Experimental rats were randomly divided into normal control group, model control group, SIL-suspension oral group, SIL-SLN oral group, and SIL-SLN intravenous （iv） group. The anti-fibrotic effects of normal drug delivery and SLN of SIL were compared. Results The SIL-SLN prepared by high pressure homogenization was spherical and regular in shape. The particle diameter was （157 ±8） nm and the zeta potentials was （-35.36± 2.68）inV. The mean entrapment efficiency was 95.64% and the mean drug content was 1. 501 g/L. After administration of SIL for 8 weeks, the gray values of Masson＇s trichrome staining in rats liver tissues of SIL-SLN oral group and SIL-SLN iv group were 4. 73± 1.35 and 2. 26 ± 0.42, respectively, and the differences were significant compared with SIL-suspension oral group （7.26± 1.72, P〈0.05）. The anti-fibrotic effect of SIL-SLN iv group was better than SIL-SLN oral group （P〈0.05）. Conclusion The anti-fibrotic effect of SIL-SLN was much higher than SIL-suspension, especially by intravenous injection. SLN is a new targeting drug delivery of traditional Chinese medicines.

关 键 词：水飞蓟宾 固体脂质纳米粒 肝纤维化 高压乳匀法 中药现代化 

分 类 号：R975[医药卫生—药品]