title: Which one performs better for targeted lung cancer combination therapy: pre- or post-bombesin-decorated nanostructured lipid carriers?
abstract: OBJECTIVE
  The co-delivery of gene and drugs has the potential to treat cancer. The aim of this study was to compare post-bombesin decorated nanostructured lipid carriers (NLC) carrying both doxorubicin (DOX) and DNA with pre-bombesin decorated NLC for lung cancer therapy.
  
  
  METHODS
  Post-bombesin decorated NLC were prepared by two steps. First, DOX and DNA-loaded NLC (DOX-DNA-NLC) was prepared. Second, Bombesin-NH2 (BN-NH2) was added into DOX-DNA-NLC to react with stearic acid-polyethylene glycol-COOH (SA-PEG-COOH) loaded in NLC. Pre-bombesin decorated NLC were prepared by two steps. First, Bombesin (BN)-conjugated ligands were synthesized. Second, DOX and DNA were loaded into BN decorated NLC. Their average size, zeta potential, drug and gene loading were evaluated. NCl-H460 human non-small lung cancer cells (NCl-H460 cells) were used for the testing of in vitro transfection efficiency and in vitro cytotoxicity. In vivo transfection efficiency and anti-tumor effect of NLC were evaluated on mice bearing NCl-H460 cells model.
  
  
  RESULTS
  Post-bombesin decorated NLC has a particle size of 128 nm, DOX encapsulation efficiency (EE) of 85% and DNA EE of 91%. Pre-bombesin decorated NLC has a particle size of 101 nm, DOX EE of 86% and DNA EE of 92%. Post-bombesin decorated NLC displayed more stable and remarkably higher transfection efficiency and better anti-tumor ability than pre-bombesin decorated NLC both in vitro and in vivo.
  
  
  CONCLUSIONS
  Post-bombesin decorated NLC could function as better carriers to improve the cell targeting and nuclear targeting ability. The resulting nanomedicine could be a promising active targeting drug/gene therapeutic system for lung cancer therapy.
authors.affiliation: a Department of Thoracic Surgery , Linyi People's Hospital , Linyi , China and.
authors.forename: Jiahui
authors.initials: J
authors.lastname: Du
authors.affiliation: b Department of Clinical Laboratory , Linyi Cancer Hospital , Linyi , China.
authors.forename: Ling
authors.initials: L
authors.lastname: Li
mesh_terms: D000818:Animals; D001839:Bombesin / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004247:DNA; D018736:DNA Adducts / Q000737:chemistry / Q000494:pharmacology*; D004317:Doxorubicin / Q000737:chemistry / Q000494:pharmacology*; D004337:Drug Carriers; D016503:Drug Delivery Systems; D006801:Humans; D008175:Lung Neoplasms / Q000737:chemistry / Q000188:drug therapy*; D051379:Mice; D049329:Nanostructures / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry* / Q000627:therapeutic use; D013229:Stearic Acids / Q000737:chemistry* / Q000494:pharmacology; D014162:Transfection
chemical_list: D018736:DNA Adducts; D004337:Drug Carriers; D013229:Stearic Acids; C031902:doxorubicin-DNA; D011092:Polyethylene Glycols; C031183:stearic acid; D004317:Doxorubicin; D004247:DNA; D001839:Bombesin
keywords: Bombesin; lung cancer; nanostructured lipid carriers; post-decorated; targeting