摘要
目的评价水飞蓟素肠溶PLGA纳米粒口服给药后在大鼠体内的分布及肝靶向效率。方法以水飞蓟素分散片为对照,大鼠灌胃给药给予水飞蓟素肠溶PLGA纳米粒和水飞蓟素PLGA纳米粒后,采用高效液相色谱法测定血浆及各组织匀浆液中的药物浓度,采用DAS 3.0计算AUC值,以相对靶向效率(RTE)和肝靶向效率(TE)评价各制剂对肝脏的靶向性。结果以水飞蓟素分散片为对照,水飞蓟素肠溶PLGA纳米粒和水飞蓟素PLGA纳米粒给药后,血浆及各组织的RTE值均大于1,肝脏RTE值均大于10;两种纳米粒制剂给药后,肝脏相对于血浆及各组织TE值均大于1.5。结论水飞蓟素肠溶PLGA纳米粒大鼠给药后能有效提高其体内吸收和组织分布,具有良好的肝靶向作用。
Objective To evaluate the body tissue distribution and liver targeting efficiency of silymarin carried by enterie coated poly（ lactic-co-glycolie acid） （PLGA） nanoparticles in rats. Methods High performance liquid chromatography （HPLC） was established and used to determinate silymarin concentration in plasma and tissue samples. The rats were randomized into 3 groups based on the treatment： enteric coated silymarin-PLGA nanoparticles, silymarin-PLGA nanoparticles and silymarin dispersible tablets （control）. DAS 3.0 was used to calculate the area under the curve （AUC）. Relative targeting efficiency （RTE） and liver targeting effieiency （TE） were used to evaluate liver targeting distribution of each agent. Results Comparing with silymarin dispersible tablets, the RTE value in the plasma and tissues was greater than 1 and the liver RTE value was greater than 10 after administrated with enteric coated and non-coated silymarin-PLGA nanoparticles. In both groups treated with silymarin-PLGA nanoparticles, the liver TE value was greater than 1.5 then compared with the TE values of plasma and other tissues. Conclusion Oral administration of enteric coated silymarin-PLGA nanoparticles improves the absorption and tissue distribution of silymarin in rats, exerting a better liver targeting efficiency.
出处
《第三军医大学学报》
CAS
CSCD
北大核心
2016年第18期2036-2040,共5页
Journal of Third Military Medical University
基金
重庆市科技攻关计划项目(CSTC2012gg-yyjs10008)~~
关键词
水飞蓟素
肠溶PLGA纳米粒
组织分布
肝靶向作用
silymarin
enteric coated silymarin-PLGA nanoparticle
tissue distribution
liver targeting
