title: The anti-tumor performance of docetaxel liposomes surface-modified with glycyrrhetinic acid.
abstract: OBJECTIVE
  Anti-tumor performance of docetaxel liposomes surface-modified with glycyrrhetinic acid (GA-DX-Lip) as a new hepatocytes-targeted delivery vehicle was investigated, unmodified docetaxel liposome (DX-Lip) was chosen as a comparison.
  
  
  METHODS
  GA-DX-Lip was prepared by film dispersion method. The physicochemical properties were characterized. The cellular uptake mechanism of GA-modified liposomes was studied in hepatocytes and nonparenchymal cells. Pharmacokinetics and the anti-tumor activity in vitro and in vivo of GA-DX-Lip were investigated.
  
  
  RESULTS
  The size of GA-DX-Lip was about 90 nm with negative charge and the entrapment efficiency was more than 95%. GA-modified liposomes had the specific receptor-mediated cellular endocytosis to hepatocytes, and the uptake ratio of hepatocytes to nonparenchymal cells was 2.28 times. The tumor inhibitory ratio of GA-DX-Lip in vitro was 2.03 times of DX-Lip, the T/C of GA-DX-Lip was 20.14%, better than the 33.27% of DX-Lip. There was no obvious difference in pharmacokinetics parameters.
  
  
  CONCLUSIONS
  The preliminary cellular uptake test showed the receptor-mediated endocytosis and enhanced hepatocytes-target for GA-modified liposomes. Compared with the unmodified liposome, GA-DX-Lip possessed better anti-tumor activity and unchanged pharmacokinetic behavior. The present results suggest that the GA-modified liposomes may be a promising delivery system for hepatocytes-target.
authors.affiliation: Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, China.
authors.forename: Jie
authors.initials: J
authors.lastname: Li
authors.forename: Haie
authors.initials: H
authors.lastname: Xu
authors.forename: Xue
authors.initials: X
authors.lastname: Ke
authors.forename: Jilai
authors.initials: J
authors.lastname: Tian
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy / Q000473:pathology; D002460:Cell Line; D000077143:Docetaxel; D016503:Drug Delivery Systems; D004705:Endocytosis; D005260:Female; D006034:Glycyrrhetinic Acid / Q000737:chemistry*; D056945:Hep G2 Cells; D022781:Hepatocytes / Q000378:metabolism; D006801:Humans; D008081:Liposomes; D008099:Liver / Q000166:cytology / Q000378:metabolism; D008113:Liver Neoplasms / Q000188:drug therapy / Q000473:pathology; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D043823:Taxoids / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D008081:Liposomes; D043823:Taxoids; D000077143:Docetaxel; D006034:Glycyrrhetinic Acid