title: Brucine-loaded liposomes composed of HSPC and DPPC at different ratios: in vitro and in vivo evaluation.
abstract: OBJECTIVE
  The objective of this study is to test the hypothesis that the phase transition temperature (T(m)), the main property of liposomes, can be easily controlled by changing the molar ratio of hydrogenated soy phosphatidylcholine (HSPC) and 1,2-dipalmitoyl-sn-glycero-3-phosphacholine (DPPC) after drug encapsulation.
  
  
  METHODS
  Brucine, an antitumor alkaloid, was encapsulated into the liposomes with different HSPC/DPPC compositions. The T(m)s of the brucine-loaded liposomes (BLs) were determined by differential scanning calorimetry (DSC). Then the physicochemical properties and pharmacokinetics of the BLs with different HSPC/DPPC compositions were investigated and compared.
  
  
  RESULTS
  The results of DSC revealed that HSPC and DPPC can combine into one phase. The findings of molecular modeling study suggested that HSPC interacts with DPPC via electrostatic interaction. The molar ratio of HSPC/DPPC influenced the sizes of BLs but had little effect on the entrapment efficiency (EE). The stability of BLs was improved with the increase of the HSPC ratios, especially with the presence of plasma. Following i.v. administration, it was found that AUC values of BLs in vivo were directly related to the HSPC/DPPC ratios of BLs, namely the T(m)s of BLs.
  
  
  CONCLUSIONS
  The behavior of liposomes, especially in vivo pharmacokinetic behavior, can be controlled by the modification of T(m).
  
  
  CONCLUSIONS
  The characterization of BLs in vitro and in vivo had demonstrated that the Tm could be flexibly modified for liposomes composed of both HSPC and DPPC. Using HSPC/DPPC composition may be an efficient strategy to control the T(m), thus control the in vivo pharmacokinetic behavior, of BLs.
authors.affiliation: National First-Class Key Discipline for Traditional Chinese Medicine, Nanjing University of Chinese Medicine , Nanjing , P.R. China .
authors.forename: Jun
authors.initials: J
authors.lastname: Chen
authors.forename: Chao-Qin
authors.initials: CQ
authors.lastname: He
authors.forename: Ai-Hua
authors.initials: AH
authors.lastname: Lin
authors.forename: Fei
authors.initials: F
authors.lastname: Xu
authors.forename: Fang
authors.initials: F
authors.lastname: Wang
authors.forename: Bo
authors.initials: B
authors.lastname: Zhao
authors.forename: Xiao
authors.initials: X
authors.lastname: Liu
authors.forename: Zhi-Peng
authors.initials: ZP
authors.lastname: Chen
authors.forename: Bao-chang
authors.initials: BC
authors.lastname: Cai
mesh_terms: D015060:1,2-Dipalmitoylphosphatidylcholine / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry*; D000818:Animals; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006865:Hydrogenation; D008081:Liposomes; D008297:Male; D010713:Phosphatidylcholines / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry; D011897:Random Allocation; D051381:Rats; D017207:Rats, Sprague-Dawley; D013025:Glycine max / Q000737:chemistry*; D013331:Strychnine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000737:chemistry
chemical_list: D008081:Liposomes; D010713:Phosphatidylcholines; D015060:1,2-Dipalmitoylphosphatidylcholine; C083806:brucine; D013331:Strychnine