title: Preparation and property analysis of a hepatocyte targeting pH-sensitive liposome.
abstract: OBJECTIVE
  To develop a hepatocyte targeting pH-sensitive liposome for drug delivery based on active targeting technology mediated by asialoglycoprotein receptors.
  
  
  METHODS
  Four types of targeting molecules with galactose residue were synthesized and mixed with pH-sensitive lipids DC-chol/DOPE to prepare liposome with integrated property of hepatocyte specificity and pH sensitivity. Liposome 18-gal was selected with the best transfection activity through cellular uptake experiment. Property analysis was made through experiments of competitive inhibition of receptors, red blood cell hemolysis, in vitro cytotoxicity test by MTS assay and mediation of inhibitory effects of antisense phosphorothioate ODN on gene expression, etc.
  
  
  RESULTS
  Liposome 18-gal had the desired properties of hepatocyte specificity, pH sensitivity, low cytotoxicity, and high transfection efficiency.
  
  
  CONCLUSIONS
  Liposome 18-gal can be further developed as a potential hepatocyte- targeting delivery system.
authors.affiliation: Beijing Institute of Radiation Medicine, Beijing 100850, China.
authors.forename: Si-Yuan
authors.initials: SY
authors.lastname: Wen
authors.forename: Xiao-Hong
authors.initials: XH
authors.lastname: Wang
authors.forename: Li
authors.initials: L
authors.lastname: Lin
authors.forename: Wei
authors.initials: W
authors.lastname: Guan
authors.forename: Sheng-Qi
authors.initials: SQ
authors.lastname: Wang
mesh_terms: D045744:Cell Line, Tumor; D016503:Drug Delivery Systems / Q000379:methods*; D022781:Hepatocytes / Q000378:metabolism*; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008081:Liposomes / Q000493:pharmacokinetics* / Q000633:toxicity; D008113:Liver Neoplasms; D009841:Oligonucleotides / Q000493:pharmacokinetics; D010957:Plasmids / Q000493:pharmacokinetics; D012680:Sensitivity and Specificity; D014162:Transfection / Q000379:methods*
chemical_list: D008081:Liposomes; D009841:Oligonucleotides