title: Folate-polyethylene glycol conjugated near-infrared fluorescence probe with high targeting affinity and sensitivity for in vivo early tumor diagnosis.
abstract: OBJECTIVE
  The purpose of this study is to synthesize a folate-polyethylene glycol (PEG) conjugated near-infrared fluorescence probe (fPI-01) for diagnosis of folate receptor (FR)-overexpressed tumors with high sensitivity and specificity.
  
  
  METHODS
  fPI-01 was synthesized, purified, and characterized. Its cytotoxicity and affinity to tumor cells were determined in vitro. The dynamics and biodistribution of the probe was monitored in normal nude mice. And the tumor-targeting capability was investigated in nude mice bearing different tumor xenograft.
  
  
  RESULTS
  fPI-01 was successfully synthesized with strengthened optical properties. Cells experiments showed the probe had high FR affinity and without apparent cytotoxicity. Animal experiments indicated the probe excreted through urine by kidney. And its tumor-targeting ability was demonstrated on different tumor-bearing mice, with high sensitivity and tumor-to-normal tissue contrast ratio (10:1).
  
  
  CONCLUSIONS
  fPI-01 is a promising optical agent for diagnosis of FR-positive tumors, especially in their early stage.
authors.affiliation: Department of Biomedical Engineering, School of Life Science and Technology, China Pharmaceutical University, Nanjing, People's Republic of China.
authors.forename: Fei
authors.initials: F
authors.lastname: Liu
authors.forename: Dawei
authors.initials: D
authors.lastname: Deng
authors.forename: Xinyang
authors.initials: X
authors.lastname: Chen
authors.forename: Zhiyu
authors.initials: Z
authors.lastname: Qian
authors.forename: Samuel
authors.initials: S
authors.lastname: Achilefu
authors.forename: Yueqing
authors.initials: Y
authors.lastname: Gu
mesh_terms: D000818:Animals; D016503:Drug Delivery Systems; D055088:Early Detection of Cancer / Q000295:instrumentation / Q000379:methods; D005260:Female; D005456:Fluorescent Dyes / Q000008:administration & dosage; D005492:Folic Acid / Q000008:administration & dosage / Q000737:chemistry*; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D008297:Male; D051379:Mice; D008819:Mice, Nude; D008954:Models, Biological; D015335:Molecular Probes / Q000008:administration & dosage / Q000737:chemistry; D009369:Neoplasms / Q000175:diagnosis*; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000737:chemistry*; D051381:Rats; D012680:Sensitivity and Specificity; D019265:Spectroscopy, Near-Infrared / Q000295:instrumentation / Q000379:methods*; D013379:Substrate Specificity; D014407:Tumor Cells, Cultured
chemical_list: D005456:Fluorescent Dyes; D015335:Molecular Probes; D011092:Polyethylene Glycols; D005492:Folic Acid