title: Brain targeting studies on buspirone hydrochloride after intranasal administration of mucoadhesive formulation in rats.
abstract: OBJECTIVE
  The purpose of this study was to find out whether nasal application of buspirone could increase its bioavailability and directly transport the drug from nose to brain.
  
  
  METHODS
  A nasal formulation (Bus-chitosan) was prepared by dissolving 15.5 mg buspirone hydrochloride, 1% w/v chitosan hydrochloride and 5% w/v hydroxypropyl beta-cyclodextrin (HP-beta-CD) in 5 ml of 0.5% sodium chloride solution. The formulation was nasally administered to rats and the plasma and brain concentration compared with that for buspirone hydrochloride solution after intravenous and intranasal (Bus-plain) administration. The brain drug uptake was also confirmed by gamma scintigraphic study.
  
  
  RESULTS
  The nasal Bus-chitosan formulation improved the absolute bioavailability to 61% and the plasma concentration peaked at 30 min whereas the peak for nasal Bus-plain formulation was 60 min. The AUC0-480 in brain after nasal administration of Bus-chitosan formulation was 2.5 times that obtained by intravenous administration (711+/-252 ng/g vs 282+/-110 ng/g); this was also considerably higher than that obtained with the intranasal Bus-plain formulation (354+/-80 ng/g). The high percentage of direct drug transport to the brain (75.77%) and high drug targeting index (>1) confirmed the direct nose to brain transport of buspirone following nasal administration of Bus-chitosan formulation.
  
  
  CONCLUSIONS
  These results conclusively demonstrate increased access of buspirone to the blood and brain from intranasal solution formulated with chitosan and HP-beta-CD.
authors.affiliation: Institute of Pharmaceutical Education and Research (IPER), Maharashtra, India. shaguftakhan17@rediffmail.com
authors.forename: Shagufta
authors.initials: S
authors.lastname: Khan
authors.forename: Kundan
authors.initials: K
authors.lastname: Patil
authors.forename: Pramod
authors.initials: P
authors.lastname: Yeole
authors.forename: Rajiv
authors.initials: R
authors.lastname: Gaikwad
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000269:Adhesives; D000281:Administration, Intranasal; D000818:Animals; D014151:Anti-Anxiety Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D001682:Biological Availability; D001692:Biological Transport; D001921:Brain / Q000378:metabolism*; D002065:Buspirone / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D048271:Chitosan; D004337:Drug Carriers; D004339:Drug Compounding; D007275:Injections, Intravenous; D008297:Male; D009297:Nasal Mucosa / Q000378:metabolism*; D051381:Rats; D017208:Rats, Wistar; D012996:Solutions; D047392:beta-Cyclodextrins
chemical_list: D000269:Adhesives; D014151:Anti-Anxiety Agents; D004337:Drug Carriers; D012996:Solutions; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D048271:Chitosan; D002065:Buspirone