title: Dual ligands modified double targeted nano-system for liver targeted gene delivery.
abstract: BACKGROUND
  It is now well established that the surface of nanocarriers with specific ligands defines a new biological identity, which assist in targeting and internalization of the nanocarriers to specific cell populations, such as cancers and disease organs.
  
  
  OBJECTIVE
  The aim of this study is to develop systemically administrable dual ligands modified nano-system which could both target cancer cells and macrophages in the liver.
  
  
  METHODS
  Transferrin (Tf) and mannan (M) were linked onto polyethylene glycol-phosphatidylethanolamine (PEG-PE) and PE separately to get transferrin-PEG-PE (T-PEG-PE) and mannan-PE (M-PE) ligands for the surface modification of carriers. The in vivo transfection efficiency of the novel dual ligands modified (D-modified) vectors were evaluated in tumor bearing animal models.
  
  
  RESULTS
  D-modified solid lipid nanoparticles/enhanced green fluorescence protein plasmid (D-SLN/pEGFP) has a particle size of 198 nm and a gene loading quantity of 89%. D-SLN/pEGFP displayed over 25% higher transfection efficiency than M-PE modified SLN/pEGFP (M-SLN/pEGFP) in HepG2 cells and T-PEG-PE modified SLN/pEGFP (T-SLN/pEGFP) in Kupffer cells (KCs) isolated from mice.
  
  
  CONCLUSIONS
  It could be concluded that T-PEG-PE and M-PE could function as excellent active targeting ligands to improve the cell targeting ability of the carriers and the dual ligands modified vectors could be applied as a promising active targeting gene delivery system.
authors.affiliation: Department of Pharmacy, The Affiliated Hospital of Medical College, Qingdao University, Qingdao, China. fanbo.jing@yahoo.com.cn
authors.forename: Fanbo
authors.initials: F
authors.lastname: Jing
authors.forename: Jing
authors.initials: J
authors.lastname: Li
authors.forename: Donghua
authors.initials: D
authors.lastname: Liu
authors.forename: Chenjing
authors.initials: C
authors.lastname: Wang
authors.forename: Zhongguo
authors.initials: Z
authors.lastname: Sui
mesh_terms: D000818:Animals; D004195:Disease Models, Animal; D018014:Gene Transfer Techniques; D015316:Genetic Therapy / Q000379:methods; D005822:Genetic Vectors / Q000008:administration & dosage / Q000737:chemistry; D049452:Green Fluorescent Proteins / Q000235:genetics*; D056945:Hep G2 Cells; D006801:Humans; D007728:Kupffer Cells / Q000378:metabolism; D008024:Ligands; D008099:Liver / Q000378:metabolism*; D008264:Macrophages / Q000378:metabolism; D008351:Mannans / Q000737:chemistry; D051379:Mice; D008807:Mice, Inbred BALB C; D053758:Nanoparticles; D010316:Particle Size; D010714:Phosphatidylethanolamines / Q000737:chemistry; D010957:Plasmids; D011092:Polyethylene Glycols / Q000737:chemistry; D014162:Transfection; D014168:Transferrin / Q000737:chemistry
chemical_list: D008024:Ligands; D008351:Mannans; D010714:Phosphatidylethanolamines; D014168:Transferrin; C485184:enhanced green fluorescent protein; D049452:Green Fluorescent Proteins; C483858:phosphatidylethanolamine; D011092:Polyethylene Glycols