title: Design, characterization, and evaluation of intranasal delivery of ropinirole-loaded mucoadhesive nanoparticles for brain targeting.
abstract: BACKGROUND
  Parkinson disease (PD) is a common, progressive neurodegenerative disorder, characterized by marked depletion of striatal dopamine and degeneration of dopaminergic neurons in the substantia nigra.
  
  
  OBJECTIVE
  The purpose of the present study was to investigate the possibility of targeting an anti-Parkinson's drug ropinirole (RH) to the brain using polymeric nanoparticles.
  
  
  METHODS
  Ropinirole hydrochloride (RH)-loaded chitosan nanoparticles (CSNPs) were prepared by an ionic gelation method. The RH-CSNPs were characterized for particle size, polydispersity index (PDI), zeta potential, loading capacity, entrapment efficiency in vitro release study, and in vivo distribution after intranasal administration.
  
  
  CONCLUSIONS
  The RH-CSNPs showed sustained release profiles for up to 18 h. The RH concentrations (% Radioactivity/g) in the brain following intranasal administration (i.n.) of RH-CSNPs were found to be significantly higher at all the time points compared with RH solution. The concentration of RH was highest in the liver (7.210 ± 0.52), followed by kidneys (6.862 ± 0.62), intestine (4.862 ± 0.45), and lungs (4.640 ± 0.92) in rats following i.n. administration of RH-CSNPs. Gamma scintigraphy imaging in rats was performed to ascertain the localization of drug in the brain following intranasal administration of formulations. The brain/blood ratios obtained (0.251 ± 0.09 and 0.386 ± 0.57 of RH (i.n.) and RH-CSNPs (i.n.), respectively) at 0.5 h are indicative of direct nose to brain transport, bypassing the blood-brain barrier (BBB).
  
  
  CONCLUSIONS
  The novel formulation showed the superiority of nose to brain delivery of RH using mucoadhesive nanoparticles compared with other delivery routes reported earlier.
authors.affiliation: a Department of Pharmaceutics, Faculty of Pharmacy , Jamia Hamdard , Hamdard Nagar , New Delhi , India .
authors.forename: Omidreza
authors.initials: O
authors.lastname: Jafarieh
authors.affiliation: a Department of Pharmaceutics, Faculty of Pharmacy , Jamia Hamdard , Hamdard Nagar , New Delhi , India .|b Department of Pharmaceutical Technology, School of Pharmacy , International Medical University (IMU) , Bukit Jalil , Kuala Lumpur , Malaysia .
authors.forename: Shadab
authors.initials: S
authors.lastname: Md
authors.affiliation: a Department of Pharmaceutics, Faculty of Pharmacy , Jamia Hamdard , Hamdard Nagar , New Delhi , India .
authors.forename: Mushir
authors.initials: M
authors.lastname: Ali
authors.affiliation: a Department of Pharmaceutics, Faculty of Pharmacy , Jamia Hamdard , Hamdard Nagar , New Delhi , India .
authors.forename: Sanjula
authors.initials: S
authors.lastname: Baboota
authors.affiliation: a Department of Pharmaceutics, Faculty of Pharmacy , Jamia Hamdard , Hamdard Nagar , New Delhi , India .|c Department of Pharmaceutics , Khalsa College of Pharmacy , Amritsar , India .
authors.forename: J K
authors.initials: JK
authors.lastname: Sahni
authors.affiliation: a Department of Pharmaceutics, Faculty of Pharmacy , Jamia Hamdard , Hamdard Nagar , New Delhi , India .|d Department of Pharmaceutics , Dehradun Institute of Technology (DIT) , Dehradun , Uttaranchal , India , and.
authors.forename: Bhavna
authors.initials: B
authors.lastname: Kumari
authors.affiliation: e Department of Radiopharmaceuticals , Institute of Nuclear Medicine and Allied Sciences (INMAS) , New Delhi , India.
authors.forename: Aseem
authors.initials: A
authors.lastname: Bhatnagar
authors.affiliation: a Department of Pharmaceutics, Faculty of Pharmacy , Jamia Hamdard , Hamdard Nagar , New Delhi , India .
authors.forename: Javed
authors.initials: J
authors.lastname: Ali
mesh_terms: D000268:Adhesiveness; D000281:Administration, Intranasal; D000818:Animals; D000978:Antiparkinson Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D001921:Brain / Q000378:metabolism; D048271:Chitosan / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers / Q000737:chemistry; D065546:Drug Liberation; D007211:Indoles / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D008297:Male; D053758:Nanoparticles / Q000737:chemistry*; D010300:Parkinson Disease / Q000188:drug therapy; D010316:Particle Size; D011877:Radionuclide Imaging; D051381:Rats; D013499:Surface Properties; D013552:Swine; D013678:Technology, Pharmaceutical / Q000379:methods
chemical_list: D000978:Antiparkinson Agents; D004337:Drug Carriers; D007211:Indoles; C046649:ropinirole; D048271:Chitosan
keywords: Brain targeting; Parkinson’s disease; biodistribution; gamma scintigraphy; nanoparticles