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Molecules 2015, 20(4), 5889-5907; doi:10.3390/molecules20045889

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

1
School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China
2
National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herb Medicine, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 13 February 2015 / Revised: 18 March 2015 / Accepted: 30 March 2015 / Published: 3 April 2015
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [1630 KB, uploaded 3 April 2015]   |  

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. View Full-Text
Keywords: saikosaponin a; saikosaponin d; liposomes; formulations; hemolytic; pharmacokinetic saikosaponin a; saikosaponin d; liposomes; formulations; hemolytic; pharmacokinetic
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Zhang, G.-S.; Hu, P.-Y.; Li, D.-X.; He, M.-Z.; Rao, X.-Y.; Luo, X.-J.; Wang, Y.-S.; Wang, Y.-R. Formulations, Hemolytic and Pharmacokinetic Studies on Saikosaponin a and Saikosaponin d Compound Liposomes. Molecules 2015, 20, 5889-5907.

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