title: The use of borneol as an enhancer for targeting aprotinin-conjugated PEG-PLGA nanoparticles to the brain.
abstract: OBJECTIVE
  To evaluate the effect of borneol on the brain targeting efficiency of aprotinin-conjugated poly (ethyleneglycol)-poly (L-lactic-co-glycolic acid) nanoparticles (Apr-NP) and the activity of huperzine A (Hup A) loaded nanoparticles to AD rats .
  
  
  METHODS
  Apr-NP was prepared by emulsion and solvent evaporation method. The uptake of Apr-NP alone or combined with borneol by brain capillary endothelial cells (BCECs) was evaluated by incorporating coumarin-6 as a tracer. In vivo imaging and the distribution of Hup A in the brain were measured to investigate the brain delivery of Apr-NP in rats, with or without the oral administration of borneol. Morris water maze was used to evaluate the memory improvement effect of Hup A loaded nanoparticles (Apr-NP-Hup).
  
  
  RESULTS
  Co-incubation with borneol could increase the uptake of nanoparticles by BCECs. Nanoparticles delivered into the rat brain were enhanced significantly by the co-administration of borneol. The pharmacological effects of Hup A loaded nanoparticles on improving the memory impairment of AD rats were greatly improved when combined with borneol.
  
  
  CONCLUSIONS
  Borneol is a promising enhancer for brain-targeting delivery systems. When co-administered with aprotinin-modified nanoparticles, borneol could improve the brain targeting efficiency of nanoparticles significantly.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Fudan University, 826 Zhangheng Rd., Shanghai, 201203, People's Republic of China.
authors.forename: Lin
authors.initials: L
authors.lastname: Zhang
authors.forename: Limei
authors.initials: L
authors.lastname: Han
authors.forename: Jing
authors.initials: J
authors.lastname: Qin
authors.forename: Weiyue
authors.initials: W
authors.lastname: Lu
authors.forename: Jianxin
authors.initials: J
authors.lastname: Wang
mesh_terms: D000470:Alkaloids / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use; D000544:Alzheimer Disease / Q000188:drug therapy* / Q000378:metabolism; D000818:Animals; D007611:Aprotinin / Q000737:chemistry*; D001522:Behavior, Animal / Q000187:drug effects; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D001892:Camphanes / Q000737:chemistry*; D042783:Endothelial Cells / Q000378:metabolism; D008297:Male; D018782:Maze Learning / Q000187:drug effects; D051379:Mice; D008819:Mice, Nude; D058726:Nanoconjugates / Q000737:chemistry*; D018696:Neuroprotective Agents / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use; D011091:Polyesters / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012717:Sesquiterpenes / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use; D014018:Tissue Distribution
chemical_list: D000470:Alkaloids; D001892:Camphanes; D058726:Nanoconjugates; D018696:Neuroprotective Agents; D011091:Polyesters; D012717:Sesquiterpenes; C558447:methoxypolyethyleneglycol-poly(lactic-co-glycolic acid); C050426:huperzine A; D011092:Polyethylene Glycols; D007611:Aprotinin; C022871:isoborneol