title: Novel RGD containing, temozolomide-loading nanostructured lipid carriers for glioblastoma multiforme chemotherapy.
abstract: BACKGROUND
  Glioblastoma multiforme (GBM) is the most common malignant brain tumor originating in the central nervous system. Efficient delivery of therapeutic molecules to the cells and tissues is a difficult challenge.
  
  
  OBJECTIVE
  Arginine-glycine-aspartic acid peptide (RGD)-modified nanostructured lipid carriers (NLCs) were used for the delivery of temozolomide (TMZ) into the GBM to provide a new paradigm in gliomatosis cerebri treatment.
  
  
  METHODS
  RGD-conjugated polyethylene glycol-b-distearoylphosphatidylethanolamine (PEG-DSPE) was synthesized. RGD containing, TMZ-loaded NLCs (RGD-TMZ/NLCs) were prepared. Their particle size, zeta potential, drug encapsulation efficiency (EE) and drug release behavior were evaluated. In vitro cytotoxicity study of TMZ/NLCs was tested in U87 malignant glioma cells (U87MG cells). In vivo antitumor efficacy of the carriers was evaluated on mice bearing GBM model.
  
  
  RESULTS
  The U87MG cells were successfully inhibited by RGD-TMZ/NLCs in vitro. RGD-TMZ/NLCs also displayed the highest antitumor efficacy in vivo than all the other formulations used for comparison.
  
  
  CONCLUSIONS
  RGD-TMZ/NLCs were efficient in selective delivery of TMZ into U87MG cells, and inhibition efficacy is high. These RGD-modified vectors could be a superior drug delivery nano-system to achieve therapeutic efficacy, and this research could be a new promising strategy for treatment in malignant gliomatosis cerebri.
authors.affiliation: a Department of Neurosurgery , Second Affiliated Hospital, Nanchang University , Nanchang , Jiangxi , China.
authors.forename: Shuxin
authors.initials: S
authors.lastname: Song
authors.affiliation: a Department of Neurosurgery , Second Affiliated Hospital, Nanchang University , Nanchang , Jiangxi , China.
authors.forename: Guohua
authors.initials: G
authors.lastname: Mao
authors.affiliation: a Department of Neurosurgery , Second Affiliated Hospital, Nanchang University , Nanchang , Jiangxi , China.
authors.forename: Jiansheng
authors.initials: J
authors.lastname: Du
authors.affiliation: a Department of Neurosurgery , Second Affiliated Hospital, Nanchang University , Nanchang , Jiangxi , China.
authors.forename: Xingen
authors.initials: X
authors.lastname: Zhu
mesh_terms: D000818:Animals; D001932:Brain Neoplasms / Q000188:drug therapy*; D045744:Cell Line, Tumor; D003606:Dacarbazine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D005909:Glioblastoma / Q000188:drug therapy*; D005910:Glioma / Q000188:drug therapy*; D008055:Lipids / Q000737:chemistry*; D051379:Mice; D049329:Nanostructures / Q000737:chemistry*; D010714:Phosphatidylethanolamines / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D000077204:Temozolomide; D023041:Xenograft Model Antitumor Assays
chemical_list: D004337:Drug Carriers; D008055:Lipids; D010714:Phosphatidylethanolamines; C107570:polyethylene glycol-distearoylphosphatidylethanolamine; D011092:Polyethylene Glycols; D003606:Dacarbazine; D000077204:Temozolomide
keywords: Central nervous system; RGD; chemotherapy; glioblastoma multiforme; nanostructured lipid carriers