Formulations, Hemolytic and Pharmacokinetic Studies on Saikosaponin a and Saikosaponin d Compound Liposomes

Molecules

Guo-Song Zhang¹  Peng-Yi Hu¹  Dong-Xun Li²  Ming-Zhen He²  Xiao-Yong Rao²  Xiao-Jian Luo²  Yue-Sheng Wang²  Yu-Rong Wang¹ 

[1] School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China; E-Mails:;National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herb Medicine, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China; E-Mails:

关键词: saikosaponin a;    saikosaponin d;    liposomes;    formulations;    hemolytic;    pharmacokinetic;   

DOI  :  10.3390/molecules20045889

来源: mdpi

【 摘 要 】

The aim of this study was to develop and optimise a saikosaponin a and saikosaponin d compound liposome (SSa-SSd-Lip) formulation with reduced hemolysis and enhanced bioavailability. A screening experiment was done with Plackett–Burman design, and response surface methodology of five factors (EPC/SSa-SSd ratio, EPC/Chol ratio, water temperature, pH of PBS, and ultrasound time) was employed to optimise the mean diameter, entrapment efficiency of SSa and SSd, and the reduction of hemolysis for SSa-SSd-Lip. Under the optimal process conditions (EPC/SSa-SSd ratio, EPC/Chol ratio, water temperature and pH of PBS were 26.71, 4, 50 °C and 7.4, respectively), the mean diameter, the entrapment efficiency of SSa, the entrapment efficiency of SSd and the hemolysis were 203 nm, 79.87%, 86.19%, 25.16% (SSa/SSd 12.5 mg/mL), respectively. The pharmacokinetic studies showed that the SSa-SSd-Lip had increased circulation time, decreased Cl, and increased AUC, MRT and T_1/2β (p < 0.05) for both SSa and SSd after intravenous administration in comparison with solution.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.