title: Liposomes modified with YIGSR peptide for tumor targeting.
abstract: YIGSR peptide anchored sterically stabilized liposomes (YIGSR-SL) were investigated for selective and preferential presentation of carrier contents at angiogenic endothelial cells overexpressing laminin receptors on and around tumor tissue and thus for assessing their targetabilty. In vitro endothelial cell binding of liposomes exhibited 7-fold higher binding of YIGSR-SL to HUVEC in comparison to the nontargeted sterically stabilized liposomes (SL). Spontaneous lung metastasis and angiogenesis assays show that YIGSR peptide anchored liposomes are significantly (P <or= 0.01) effective in the prevention of lung metastasis and angiogenesis compared to free 5-fluorouracil (5-FU) and SL. YIGSR-SL was very effective in regression of tumors in BALB/c mice bearing B16F10 melanoma cells. Results indicate that YIGSR peptide anchored sterically stabilized liposomes bearing 5-FU are significantly (P <or= 0.01) active against primary tumor and metastasis than the SL and free drug. Thus, YIGSR peptide anchored sterically stabilized liposomes hold potential of targeted cancer chemotherapeutics.
authors.affiliation: Novel Drug Delivery Systems Laboratory, Strides Arcolab Limited, Bangalore, Karnataka, India. pd.praveen@gmail.com
authors.forename: Praveen K
authors.initials: PK
authors.lastname: Dubey
authors.forename: Deepak
authors.initials: D
authors.lastname: Singodia
authors.forename: S P
authors.initials: SP
authors.lastname: Vyas
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000494:pharmacology / Q000627:therapeutic use; D002478:Cells, Cultured; D016503:Drug Delivery Systems; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects; D005472:Fluorouracil / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D008081:Liposomes; D008175:Lung Neoplasms / Q000556:secondary; D008546:Melanoma, Experimental / Q000098:blood supply / Q000188:drug therapy; D051379:Mice; D008807:Mice, Inbred BALB C; D009842:Oligopeptides / Q000008:administration & dosage* / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D000970:Antineoplastic Agents; D008081:Liposomes; D009842:Oligopeptides; C081571:tyrosyl-isoleucyl-glycyl-seryl-arginine; D005472:Fluorouracil