title: Liposomal quercetin: evaluating drug delivery in vitro and biodistribution in vivo.
abstract: OBJECTIVE
  The drug-loaded PEGylated nanomaterials have shown effective cell-killing in vitro, but to the best of authors' knowledge there have been no reports of successful drug delivery in vitro and in vivo using polyethyleneglycol-2000-distearoyl phosphatidyl ethanolamine (PEG2000-DSPE) nanomaterials loaded with unmodified drug molecules, such as quercetin (QUE). In this study, it remained an open question as to whether such formulations could prove effective in vitro and in vivo, and to study the distribution and clearance of PEG-DPSE-ylated lipid-based quercetin nanoliposomes (PEG2000-DPSE-QUE-NLs) as delivery vehicles for the anticancer drug in vitro and in vivo.
  
  
  METHODS
  PEG-DPSE layers were attached to QUE-NLs, dispersed in aqueous media and characterized using TEM and HPLC/UV spectroscopy. Tumor cell killing efficacy was assessed in vitro using MTT and trypan blue exclusion assays, and the distribution and clearance pathways, as well as repeated administration in rats, were studied by HPLC spectroscopy.
  
  
  RESULTS
  PEG2000-DPSE-QUE-NLs were efficiently dispersed in aqueous media compared with controls, and PEGylated (PEG2000-DPSE) NLs were found to be effective drug delivery vehicles when simply loaded with QUE. The plasma QUE concentration decreased significantly (p < 0.05) after repeated administration of PEG2000-DSPE liposomal QUE. There was a slight ABC phenomenon with the PEG2000-DSPE-modified QUE liposomes.
  
  
  CONCLUSIONS
  The QUE/PEG2000-DPSE formulation was more effective than QUE in vitro on inhibiting the growth of glioma cancer cells. This work demonstrates that nanomaterials (PEG2000-DPSE) are effective drug delivery vehicles in vivo as tumor-targeted drug carriers.
authors.affiliation: Hubei University of Medicine, Taihe Hospital, Department of Pharmacy, Hubei Province, People's Republic of China.
authors.forename: Wang
authors.initials: W
authors.lastname: Gang
authors.forename: Wang Jun
authors.initials: WJ
authors.lastname: Jie
authors.forename: Zhang Li
authors.initials: ZL
authors.lastname: Ping
authors.forename: Du Shi
authors.initials: du S
authors.lastname: Ming
authors.forename: Liu Ju
authors.initials: LJ
authors.lastname: Ying
authors.forename: Wang
authors.initials: W
authors.lastname: Lei
authors.forename: Ye
authors.initials: Y
authors.lastname: Fang
mesh_terms: D000825:Animal Structures; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage / Q000493:pharmacokinetics; D002470:Cell Survival; D002851:Chromatography, High Pressure Liquid; D016503:Drug Delivery Systems; D004797:Enzyme-Linked Immunosorbent Assay; D005910:Glioma / Q000188:drug therapy / Q000473:pathology; D008081:Liposomes / Q000737:chemistry*; D049329:Nanostructures / Q000737:chemistry; D010714:Phosphatidylethanolamines / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D011794:Quercetin / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution; D014407:Tumor Cells, Cultured
chemical_list: C519184:1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy-poly(ethylene glycol 2000); D000975:Antioxidants; D008081:Liposomes; D010714:Phosphatidylethanolamines; D011092:Polyethylene Glycols; D011794:Quercetin