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


CONCLUSIONS
Compared with the commercial injection, liposomes delivered more drugs into the brain and have longer elimination time.
Lv
Wenli
W
School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
Guo
Jianxin
J
Li
Jin
J
Huang
Luosheng
L
Ping
Qineng
Q
D000818:Animals; D019540:Area Under Curve; D001921:Brain / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D004339:Drug Compounding; D004355:Drug Stability; D005419:Flavonoids / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D007275:Injections, Intravenous; D008081:Liposomes; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013997:Time Factors
D005419:Flavonoids; D008081:Liposomes; C061097:breviscapine