Distribution of liposomal breviscapine in brain following intravenous injection in rats.
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.[1]References
- Distribution of liposomal breviscapine in brain following intravenous injection in rats. Lv, W., Guo, J., Li, J., Huang, L., Ping, Q. International journal of pharmaceutics. (2005) [Pubmed]
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