脂质体
丹参
化学
生物利用度
药代动力学
药理学
PEG比率
聚乙二醇
色谱法
Zeta电位
体内
磷脂酰胆碱
粒径
材料科学
生物化学
医学
纳米技术
纳米颗粒
中医药
生物
磷脂
经济
替代医学
财务
生物技术
物理化学
病理
膜
作者
Lihong Zhang,Limei Han,Xun Sun,Dongyan Gao,Jing Qin,Jianxin Wang
出处
期刊:Fitoterapia
[Elsevier]
日期:2012-06-01
卷期号:83 (4): 678-689
被引量:44
标识
DOI:10.1016/j.fitote.2012.02.004
摘要
The clinical application of salvianolic acid B (Sal B), a potential therapeutic agent for cardiovascular diseases isolated from Salvia miltiorrhiza, is greatly restricted by its short half-life and low bioavailability. To improve therapeutic effects and prolong the systemic circulation time of Sal B, liposomes, composed of soybean phosphatidylcholine and cholesterol were prepared by reverse-phase evaporation method. In addition, polyethylene glycol 2000-disteroylphosphoethanolamine (PEG-DSPE 2000) was included to give steric barrier to liposomes. A central composite design was employed to optimize liposomal formulation with high encapsulation efficiency and small particle size. Physicochemical characteristics such as particle size, zeta potential, encapsulation efficiency and in vitro release were investigated. In vivo pharmacokinetic properties of Sal B in beagle dogs and the effect of PEG on the blood circulation time of Sal B-loaded liposomes were also evaluated. An optimized formulation with encapsulation efficiency of 73.68% and mean particle size of 136.6nm were developed. Encapsulation of Sal B into conventional and PEGylated liposomes could prolong the half-life of Sal B by 5.8- and 17.5-fold and enhance the AUC(0-t) of Sal B by 6.7- and 13.3-fold compared with free Sal B, respectively. Therefore, the use of PEGylated liposomes could prolong the circulation time in blood and longevity effect of liposomes on Sal B was increased by PEG.
科研通智能强力驱动
Strongly Powered by AbleSci AI