title: Preparation of rotigotine-loaded microspheres and their combination use with L-DOPA to modify dyskinesias in 6-OHDA-lesioned rats.
abstract: OBJECTIVE
  To prepare rotigotine loaded microspheres (RoMS) to achieve continuous dopaminergic stimulation (CDS) for the treatment of Parkinson's disease (PD) and investigate both the therapeutic benefit and inducibility of AIMs of administration of RoMS combination with L-DOPA in 6-OHDA-leisioned rats.
  
  
  METHODS
  Rotigotine was encapsulated into poly(lactic-co-glycolic acid) (PLGA) microspheres by an oil-in-water emulsion solvent evaporation technique. In vitro characteristics and in vivo pharmacokinetics of RoMS either in rat blood or brain (by microdialysis) were investigated. Contraversive rotations and AIMs were observed to investigate the therapeutic benefit and the propensity to induce dyskinesia of RoMS or RoMS combination with L-DOPA in 6-OHDA-lesioned rats.
  
  
  RESULTS
  RoMS displayed continuous-release characteristics of rotigotine in animals and exhibited a steady efficacy lasted for 2 weeks in 6-OHDA-lesioned rats. No significant difference of the therapeutic benefit between the treatment of RoMS and pulsatile L-DOPA combination and mono L-DOPA was found. While the dyskinesia was significantly decreased with the treatment of RoMS and pulsatile L-DOPA combination compared to mono L-DOPA.
  
  
  CONCLUSIONS
  RoMS could supply an alternative of CDS for the treatment of PD and the study indicates a potential advantage of RoMS for the treatment of mild and advanced PD patient in combination with L-DOPA.
authors.affiliation: College of Life Science, Jilin University, NO.2699 Qianjin Street, 130012, Changchun, Jilin Province, China.
authors.forename: Aiping
authors.initials: A
authors.lastname: Wang
authors.forename: Lexi
authors.initials: L
authors.lastname: Wang
authors.forename: Kaoxiang
authors.initials: K
authors.lastname: Sun
authors.forename: Wanhui
authors.initials: W
authors.lastname: Liu
authors.forename: Chunjie
authors.initials: C
authors.lastname: Sha
authors.forename: Youxin
authors.initials: Y
authors.lastname: Li
mesh_terms: D000818:Animals; D018491:Dopamine Agonists / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D004337:Drug Carriers; D004359:Drug Therapy, Combination; D020820:Dyskinesias / Q000188:drug therapy*; D007980:Levodopa / Q000008:administration & dosage / Q000627:therapeutic use*; D008297:Male; D008863:Microspheres; D016627:Oxidopamine / Q000633:toxicity*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013764:Tetrahydronaphthalenes / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D013876:Thiophenes / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use
chemical_list: D018491:Dopamine Agonists; D004337:Drug Carriers; D013764:Tetrahydronaphthalenes; D013876:Thiophenes; D007980:Levodopa; C047508:rotigotine; D016627:Oxidopamine