title: Solid lipid nanoparticles as delivery systems for bromocriptine.
abstract: OBJECTIVE
  The present investigation describes a formulative study for the development of innovative drug delivery systems for bromocriptine.
  
  
  METHODS
  Solid lipid nanoparticles (SLN) based on different lipidic components have been produced and characterized. Morphology and dimensional distribution have been investigated by electron microscopy and Photon Correlation Spectroscopy. The antiparkinsonian activities of free bromocriptine and bromocriptine encapsulated in nanostructured lipid carriers were evaluated in 6-hydroxydopamine hemilesioned rats, a model of Parkinson's disease.
  
  
  RESULTS
  Tristearin/tricaprin mixture resulted in nanostructured lipid carriers with stable mean diameter up to 6 months from production. Bromocriptine was encapsulated with high entrapment efficiency in all of the SLN samples, particularly in the case of tristearin/tricaprin mixture. Bromocriptine encapsulation did not change nanoparticle dimensions. In vitro release kinetics based on a dialysis method demonstrated that bromocriptine was released in a prolonged fashion for 48 h. Tristearin/tricaprin nanoparticles better controlled bromocriptine release. Both free and encapsulated bromocriptine reduced the time spent on the blocks (i.e. attenuated akinesia) in the bar test, although the action of encapsulated bromocriptine was more rapid in onset and prolonged.
  
  
  CONCLUSIONS
  It can be concluded that nanostructured lipid carriers encapsulation may represent an effective strategy to prolong the half-life of bromocriptine.
authors.affiliation: Department of Pharmaceutical Sciences, University of Ferrara, 44100 Ferrara, Italy. ese@unife.it
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Esposito
authors.forename: Martina
authors.initials: M
authors.lastname: Fantin
authors.forename: Matteo
authors.initials: M
authors.lastname: Marti
authors.forename: Markus
authors.initials: M
authors.lastname: Drechsler
authors.forename: Lydia
authors.initials: L
authors.lastname: Paccamiccio
authors.forename: Paolo
authors.initials: P
authors.lastname: Mariani
authors.forename: Elisa
authors.initials: E
authors.lastname: Sivieri
authors.forename: Francesco
authors.initials: F
authors.lastname: Lain
authors.forename: Enea
authors.initials: E
authors.lastname: Menegatti
authors.forename: Michele
authors.initials: M
authors.lastname: Morari
authors.forename: Rita
authors.initials: R
authors.lastname: Cortesi
mesh_terms: D015502:Absorptiometry, Photon; D000818:Animals; D000978:Antiparkinson Agents / Q000008:administration & dosage* / Q000627:therapeutic use; D001522:Behavior, Animal / Q000187:drug effects; D001971:Bromocriptine / Q000008:administration & dosage* / Q000627:therapeutic use; D002851:Chromatography, High Pressure Liquid; D020285:Cryoelectron Microscopy; D003956:Dialysis; D016503:Drug Delivery Systems; D007700:Kinetics; D008027:Light; D008055:Lipids; D008297:Male; D008854:Microscopy, Electron; D053758:Nanoparticles; D016627:Oxidopamine; D010302:Parkinson Disease, Secondary / Q000139:chemically induced / Q000188:drug therapy; D051381:Rats; D017207:Rats, Sprague-Dawley; D012542:Scattering, Radiation; D013056:Spectrophotometry, Ultraviolet; D014280:Triglycerides; D014961:X-Ray Diffraction
chemical_list: D000978:Antiparkinson Agents; D008055:Lipids; D014280:Triglycerides; D001971:Bromocriptine; D016627:Oxidopamine; C010800:tricaprin; C022618:tristearin