title: Suppression of choroidal neovascularization by intravitreal injection of liposomal SU5416.
abstract: OBJECTIVE
  To clarify whether use of angiogenic vessel-homing peptide, Ala-Pro-Arg-Pro-Gly (APRPG)-modified liposomes encapsulating 3-([2,4-dimethylpyrrhol-5-yl] methylidenyl)-indolin-2-one (SU5416), an angiogenesis inhibitor, can inhibit the development of experimental choroidal neovascularization (CNV) in rats.
  
  
  METHODS
  Liposomes were prepared using the thin-film hydration method. To set up the rat experimental CNV model, intense fundus laser photocoagulation at 6 spots per eye was performed on pigmented rats. After photocoagulation, the rats were divided into 4 groups (6 rats in each group): an APRPG-liposomal SU5416 treatment group and control groups treated with a balanced salt solution, APRPG liposomes, or soluble SU5416. Each rat received a single intravitreal injection immediately after the injury. One week or 2 weeks after laser injury, the extent of CNV was evaluated by perfusion with high-molecular-weight fluorescein isothiocyanate-dextran.
  
  
  RESULTS
  Two weeks after injection, the CNV area was significantly (P < .05) smaller in the APRPG-liposomal SU5416-treated group compared with the CNV area in the balanced salt solution-and APRPG liposome-treated groups.
  
  
  CONCLUSIONS
  Liposomes modified by APRPG and encapsulating SU5416 constitute a potential drug formulation for CNV treatment that would require only a single intravitreal injection.
  
  
  CONCLUSIONS
  This liposomal delivery may enable the sustained release of small molecules and be a new treatment modality for CNV.
authors.affiliation: Department of Ophthalmology, Juntendo University Urayasu Hospital, Chiba, Japan. m-honda@juntendo-urayasu.jp
authors.forename: Miki
authors.initials: M
authors.lastname: Honda
authors.forename: Tomohiro
authors.initials: T
authors.lastname: Asai
authors.forename: Takuya
authors.initials: T
authors.lastname: Umemoto
authors.forename: Yoshihiko
authors.initials: Y
authors.lastname: Araki
authors.forename: Naoto
authors.initials: N
authors.lastname: Oku
authors.forename: Minoru
authors.initials: M
authors.lastname: Tanaka
mesh_terms: D020533:Angiogenesis Inhibitors / Q000008:administration & dosage*; D000818:Animals; D002232:Carbocyanines; D020256:Choroidal Neovascularization / Q000175:diagnosis / Q000188:drug therapy*; D003911:Dextrans; D004195:Disease Models, Animal; D016650:Fluorescein-5-isothiocyanate / Q000031:analogs & derivatives; D005456:Fluorescent Dyes; D007211:Indoles / Q000008:administration & dosage*; D058449:Intravitreal Injections; D008081:Liposomes; D008297:Male; D009842:Oligopeptides / Q000737:chemistry; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors; D011758:Pyrroles / Q000008:administration & dosage*; D051381:Rats; D011914:Rats, Inbred BN
chemical_list: D020533:Angiogenesis Inhibitors; D002232:Carbocyanines; D003911:Dextrans; D005456:Fluorescent Dyes; D007211:Indoles; D008081:Liposomes; D009842:Oligopeptides; D011758:Pyrroles; C490869:alanyl-prolyl-arginyl-prolyl-glycine; C015219:fluorescein isothiocyanate dextran; C024286:3,3'-dioctadecylindocarbocyanine; C116890:Semaxinib; D011505:Protein-Tyrosine Kinases; D016650:Fluorescein-5-isothiocyanate