title: Distribution of liposomal breviscapine in brain following intravenous injection in rats.
abstract: 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.
authors.affiliation: School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
authors.forename: Wenli
authors.initials: W
authors.lastname: Lv
authors.forename: Jianxin
authors.initials: J
authors.lastname: Guo
authors.forename: Jin
authors.initials: J
authors.lastname: Li
authors.forename: Luosheng
authors.initials: L
authors.lastname: Huang
authors.forename: Qineng
authors.initials: Q
authors.lastname: Ping
mesh_terms: 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
chemical_list: D005419:Flavonoids; D008081:Liposomes; C061097:breviscapine