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- Title
Formulations, Hemolytic and Pharmacokinetic Studies on Saikosaponin a and Saikosaponin d Compound Liposomes.
- Authors
Guo-Song Zhang; Peng-Yi Hu; Dong-Xun Li; Ming-Zhen He; Xiao-Yong Rao; Xiao-Jian Luo; Yue-Sheng Wang; Yu-Rong Wang
- Abstract
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 T1/2β (p < 0.05) for both SSa and SSd after intravenous administration in comparison with solution.
- Subjects
LIPOSOMES; HEMOLYSIS &; hemolysins; PHOSPHOLIPIDS; BILAYER lipid membranes; CYTOPLASM
- Publication
Molecules, 2015, Vol 20, Issue 4, p5889
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules20045889