文献类型：期刊文献

英文题名：Preparation of a novel ginkgolide B niosomal composite drug

作者：Zhou, Juntong[1];Wu, Xiao[1];Zhao, Zhanhong[2];Wang, Zhenpeng[3];Li, Shumu[3];Chen, Chang[1];Yu, Shan[1];Qu, Xintong[1];Li, Kexin[1];Tian, Ye[1];Liu, Xiaojing[1];Zhang, Gaoyu[1];Wang, Zhaoxuan[1];Li, Chi[1];Kang, Ning[1];Huo, Qing[1]

第一作者：Zhou, Juntong

通讯作者：Huo, Q[1]

机构：[1]Beijing Union Univ, Biochem Engn Coll, Dept Biomed, Beijing 100023, Peoples R China;[2]Beijing Union Univ, Sch Hosp, Beijing 100101, Peoples R China;[3]Chinese Acad Sci, Anal & Testing Ctr, Inst Chem, Beijing 100190, Peoples R China

第一机构：北京联合大学生物化学工程学院

通讯机构：[1]corresponding author), Beijing Union Univ, Biochem Engn Coll, Dept Biomed, Beijing 100023, Peoples R China.|[1141726]北京联合大学生物化学工程学院;[11417]北京联合大学;

年份：2020

卷号：18

期号：1

起止页码：1064-1074

外文期刊名：OPEN CHEMISTRY

收录：;Scopus(收录号：2-s2.0-85092248648);WOS:【SCI-EXPANDED(收录号:WOS:000565588900001)】；

基金：This research work was financially supported by the National Natural Science Foundation of China (Grant No. 11975048) and the Beijing Union University Graduate Program.

语种：英文

外文关键词：ginkgolide B; puerarin; niosome; Parkinson's disease

摘要：Ginkgolide B (GB) and Puerarin (Pue) are active pharmaceutical ingredients for the treatment of Parkinson's disease (PD); however, both are poorly water-soluble, which limits their bioavailability. The present study used the niosome vesicle encapsulation technique to prepare a novel GB composite drug. The conditions for GB-Pue niosomal complex preparation were as follows: a hydration temperature of 60 degrees C, a hydrophilic-lipophilic balance of 10.5, a drug-carrier mass ratio of 8:100, and a surfactant-cholesterol mass ratio of 1.5:1. The niosomal complex suspension was uniformly distributed and milky white in color, with no stratification over a duration of 1 month. It had an average particle size of 187.3 nm, a particle-size distribution of 0.237, a GB encapsulation efficiency (EE) of 68.2%, a GB drug-loading rate of 90.1%, a Pue EE of 40.5%, and a Pue drug-loading rate of 83.3%. The optimal storage temperature for the niosomal complex suspension was 4 degrees C. Following an intravenous injection of the niosomal complex suspension into the rat tail, the area under the curve (AUC) from 0 to 4 h was 54.1 h mu g mL(-1), with a mean residence time (MRT) of 0.96 h, a distribution half-life (T-1/12a) of 0.195 h, and a total clearance of 0.003 L h(-1) kg(-1). The AUC and MRT of the composite prescription were 1.1-and 1.4-times those of the commercial injection, respectively, showing significantly increased sustained release and bioavailability. Moreover, the distribution of GB in the brain tissue was 1.8-times that of the commercial injection. In conclusion, the novel GB niosomal composite drug, with excellent stability, improved pharmacokinetics, and brain tissue distribution, demonstrates great potential for the delivery of GB and Pue for PD therapeutics.