title: Preparation, pharmacokinetics and tumour-suppressive activity of berberine liposomes.
abstract: OBJECTIVE
  Berberine (BBR) has shown promising antitumour effects in vitro. However, intravenous administration of BBR solution is complicated by lethal adverse cardiovascular effects. The aim of this study was to prepare common and polyethylene glycol (PEG)-modified long-circulating BBR liposomes and evaluate their efficacy and safety as potential antitumour agents.
  
  
  METHODS
  Physiochemical properties of common and long-circulating BBR liposomes were characterized including particle size, Zeta potential and thermal stability. Pharmacokinetic and tissue distribution study of liposomal BBR was performed in rats and tumour-bearing nude mice, respectively. Antitumour efficacy and safety were observed in SGC-7901 tumour-xenografted mice.
  
  
  RESULTS
  Berberine liposomes showed homogenous morphology, storage stability and sustained-releasing behaviour in vitro. BBR liposomes led to significantly increased circulation retention of BBR in comparison with BBR solution. In tumour-bearing mice, BBR liposomes selectively increased BBR concentrations in the liver, spleen, lung and tumour, while conferred lower distribution to the heart and kidney. Importantly, chronic administration of BBR liposomes proved effective and safe in suppressing the tumour growth in nude mice, especially the PEG-modified long-circulating liposomes.
  
  
  CONCLUSIONS
  Our study suggested that BBR liposomes may provide a safe form of intravenous drug therapy for strengthening the antitumour effects of BBR.
authors.affiliation: Department of Pharmacy, Nanjing University of Chinese Medicine Affiliated Hospital, Nanjing, China.
authors.forename: Xinghui
authors.initials: X
authors.lastname: Wang
authors.affiliation: Department of Pharmacy, Nanjing University of Chinese Medicine Affiliated Hospital, Nanjing, China.
authors.forename: Qiong
authors.initials: Q
authors.lastname: Wang
authors.affiliation: Department of Pharmacy, Nanjing University of Chinese Medicine Affiliated Hospital, Nanjing, China.
authors.forename: Zhihui
authors.initials: Z
authors.lastname: Liu
authors.affiliation: School of Pharmacy, China Pharmaceutical University, Nanjing, China.
authors.forename: Xiao
authors.initials: X
authors.lastname: Zheng
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology*; D001599:Berberine / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology*; D008081:Liposomes / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D008081:Liposomes; D001599:Berberine; D011092:Polyethylene Glycols
keywords: antitumour; berberine; long-circulating liposomes; pharmacokinetics