Using PG-Liposome- Based System to Enhance Puerarin Liver-Targeted Therapy for Alcohol-Induced Liver Disease
Using PG-Liposome- Based System to Enhance Puerarin Liver-Targeted Therapy for Alcohol-Induced Liver Disease
复制标题
使用基于PG脂质体的系统增强葛根素肝脏靶向治疗酒精性肝病
DOI：
10.1208/s12249-015-0427-5
复制
发表时间：
2016
影响因子：
3.3
通讯作者：
Lu Cui Tao
中科院分区：
文献类型：
--
作者：
Zhao Ying Zheng;Zhang Lu;Gupta Pardeep K;Tian Fu Rong;Mao Kai Li;Qiu Kai Yan;Yang Wei;Lv Chuan Zhu;Lu Cui Tao
酒精性肝病（ALD）治疗的一个关键问题是缺乏高效的输送系统。在本研究中，制备了葛根素-丙二醇-脂质体系统，旨在将葛根素（一种异黄酮）靶向肝脏。透射电镜(TEM)结果显示脂质体呈球形，平均直径为182 nm，多分散指数为0.239。颗粒的zeta电位约为-30 mV。对葛根素的包封率在90%以上。 HpeG2 细胞中基于 MTT 的测定显示，在含有 3% 葛根素的系统浓度高达 25% 的情况下，没有显着的细胞毒性。该系统的体内性能在小鼠身上进行了研究。相对于相同剂量水平的葛根素溶液，研究了葛根素-PG-脂质体系统的药代动力学和分布。结果表明，葛根素-PG脂质体可延长药物保留时间，并减少小鼠体内葛根素的消除（脂质体系统和溶液的AUC分别为9.5和4.0 mg h L−1）。此外，丙二醇（PG）-脂质体系统增强了葛根素在肝脏和脾脏中的分布，同时减少了葛根素在其他组织中的分布。总体而言，葛根素-PG-脂质体系统对 ALD 小鼠显示出增强的治疗效果。
A critical issue for alcohol-induced liver disease (ALD) therapeutics is the lack of a highly efficient delivery system. In this study, a Puerarin-propylene glycol-liposome system was prepared for the purpose of targeting puerarin, an isoflavon, to the liver. Transmission electron microscope (TEM) results showed the liposomes to be spherical in shape with an average diameter of 182 nm with a polydispersity index of 0.239. The zeta potential of the particles was about −30 mV. The entrapment efficiency of puerarin was above 90%. MTT-based assay in HpeG2 cells showed no significant cytotoxicity in the presence of up to 25% concentration of the system containing 3% puerarin. In vivo performance of this system was studied in mice. Pharmacokinetics and distribution of puerarin-PG-liposome system was studied relative to puerarin solution at the same dose levels. The results show that puerarin-PGliposome prolonged drug retention time and decreased elimination of puerarin in mice (AUC of liposome system and solution was 9.5 and 4.0 mg h L−1, respectively). Furthermore, propylene glycol (PG)-liposome system enhanced puerarin distribution into liver and spleen, while decreasing puerarin distribution in other tissues. Overall, the puerarin-PG-liposome system showed enhanced therapeutic effect in mice with ALD.