title: Brain delivery of buspirone hydrochloride chitosan nanoparticles for the treatment of general anxiety disorder.
abstract: The present work discusses the preparation, characterization and in vivo evaluation of thiolated chitosan nanoparticles (TCS-NPs) of buspirone hydrochloride (BUH) for brain delivery through intranasal route. TCS NPs were prepared by ionic gelation method and characterized for various parameters. The NPs formed were having particle size of 226.7±2.52nm with PDI 0.483±0.031. Drug entrapment efficiency (EE) and loading capacity (LC) were found to be 81.13±2.8 and 49.67±5.5%. The cumulative percentage drug permeation through nasal mucosa was 76.21%. Bioadhesion study carried out on porcine mucin and showed a bioadhesion efficiency of 90.218±0.134%. Nose-to-brain delivery of placebo NPs was investigated by confocal laser scanning microscopy (CLSM) technique using rhodamine-123 as a marker. The brain concentration achieved after intranasal administration of TCS-NPs was 797.46±35.76ng/ml with tmax 120min which was significantly higher than achieved after intravenous administration on BUH solution 384.15±13.42ng/ml and tmax of 120min and intranasal administration of BUH solution 417.77±19.24ng/ml and tmax 60min.
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi 110062, India; Institute of Nanoscience and Technology, Phase X, Mohali, Chandigarh, Punjab, India.
authors.forename: Naimat Kalim
authors.initials: NK
authors.lastname: Bari
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi 110062, India.
authors.forename: Mohammad
authors.initials: M
authors.lastname: Fazil
authors.affiliation: Department of Pharmacology, Faculty of Pharmacy, Jamia Hamdard, New Delhi 110062, India.
authors.forename: Md Quamrul
authors.initials: MQ
authors.lastname: Hassan
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard, New Delhi 110062, India.
authors.forename: Md Rafi
authors.initials: MR
authors.lastname: Haider
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi 110062, India.
authors.forename: Bharti
authors.initials: B
authors.lastname: Gaba
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi 110062, India; Department of Pharmaceutics, Khalsa College of Pharmacy, Amritsar, India.
authors.forename: Jasjeet K
authors.initials: JK
authors.lastname: Narang
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi 110062, India.
authors.forename: Sanjula
authors.initials: S
authors.lastname: Baboota
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi 110062, India. Electronic address: javedaali@yahoo.com.
authors.forename: Javed
authors.initials: J
authors.lastname: Ali
mesh_terms: D000281:Administration, Intranasal; D000818:Animals; D014151:Anti-Anxiety Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001008:Anxiety Disorders / Q000188:drug therapy / Q000523:psychology*; D001682:Biological Availability; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D002065:Buspirone / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical; D048271:Chitosan / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry; D065546:Drug Liberation; D018782:Maze Learning / Q000187:drug effects; D015394:Molecular Structure; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D010539:Permeability; D051381:Rats; D017366:Serotonin Receptor Agonists / Q000008:administration & dosage* / Q000493:pharmacokinetics; D017550:Spectroscopy, Fourier Transform Infrared; D013552:Swine; D014961:X-Ray Diffraction
chemical_list: D014151:Anti-Anxiety Agents; D004337:Drug Carriers; D017366:Serotonin Receptor Agonists; D048271:Chitosan; D002065:Buspirone
keywords: Buspirone hydrochloride (BUH); General anxiety disorder; Intra nasal; Nanoparticles; Nose to brain; Thiolated chitosan