大鼠静脉注射后灯盏花素脂质体在脑中的分布。

Distribution of liposomal breviscapine in brain following intravenous injection in rats.

作者信息

Lv Wenli, Guo Jianxin, Li Jin, Huang Luosheng, Ping Qineng

机构信息

School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.

出版信息

Int J Pharm. 2005 Dec 8;306(1-2):99-106. doi: 10.1016/j.ijpharm.2005.09.012. Epub 2005 Nov 8.

DOI:10.1016/j.ijpharm.2005.09.012

PMID:16280216

Abstract

AIM

To investigate distribution of breviscapine in brain after intravenous (i.v.) injection of liposomes.

METHODS

Breviscapine liposomes were prepared by rotary evaporation-sonication method. Particle size, encapsulation efficiency and stability of liposomes were respectively examined. In vitro drug release was investigated in 0.9% sodium chloride at 37 degrees C. Rats were divided into two groups. Liposomes were given to one group and commercial injection (Injectio Breviscapine) was given to the other at a single dose of 28.1 mgkg(-1) i.v., respectively. Scutellarin in rat brain at different sampling time was determined by RP-HPLC. The brain concentration-time curves of breviscapine liposomes and commercial injection were constructed and pharmacokinetic parameters were calculated and compared by statistic analysis.

RESULTS

The average liposome diameter was 735+/-59 nm and encapsulation efficiency was 85.1+/-2.3%. The average accumulative release percentage of breviscapine liposomes in 0.9% sodium chloride was less than 30% within 24h. The mean concentration-time curves of breviscapine liposomes and commercial injection were both fitted to one-compartment model. There are significant difference of parameter T(1/2) and AUC(0-360) between liposome and commercial injection (p<0.05). T(1/2) of breviscapine liposomes and commercial injection were 23.13+/-7.71 and 6.27+/-1.84min, respectively. The brain AUC ratio of breviscapine liposomes to commercial injection was 443.4+/-92.3%.

CONCLUSION

Compared with the commercial injection, liposomes delivered more drugs into the brain and have longer elimination time.

摘要

目的

研究静脉注射脂质体后灯盏花素在脑中的分布情况。

方法

采用旋转蒸发-超声法制备灯盏花素脂质体。分别检测脂质体的粒径、包封率和稳定性。在37℃的0.9%氯化钠溶液中研究体外药物释放情况。将大鼠分为两组。分别以28.1mg/kg-1的单剂量静脉注射给予一组脂质体，另一组给予市售注射液（灯盏花素注射液）。采用反相高效液相色谱法测定不同采样时间大鼠脑中的灯盏乙素。构建灯盏花素脂质体和市售注射液的脑浓度-时间曲线，计算药代动力学参数并进行统计分析比较。

结果

脂质体平均直径为735±59nm，包封率为85.1±2.3%。灯盏花素脂质体在0.9%氯化钠溶液中24小时内的平均累积释放率小于30%。灯盏花素脂质体和市售注射液的平均浓度-时间曲线均符合一室模型。脂质体与市售注射液之间参数T(1/2)和AUC(0-360)有显著差异（p<0.05）。灯盏花素脂质体和市售注射液的T(1/2)分别为23.13±7.71和6.27±1.84分钟。灯盏花素脂质体与市售注射液的脑AUC比值为443.4±92.3%。