Methodology and effects of repeated intranasal delivery of DNSP-11 in a rat model of Parkinson's disease

J Neurosci Methods. 2015 Aug 15:251:120-9. doi: 10.1016/j.jneumeth.2015.05.006. Epub 2015 May 18.

Abstract

Background: To circumvent the challenges associated with delivering large compounds directly to the brain for the treatment of Parkinson's disease (PD), non-invasive procedures utilizing smaller molecules with protective and/or restorative actions on dopaminergic neurons are needed.

New method: We developed a methodology for evaluating the effects of a synthetic neuroactive peptide, DNSP-11, on the nigrostriatal system using repeated intranasal delivery in both normal and a unilateral 6-hydroxydopamine (6-OHDA) lesion rat model of PD.

Results: Normal rats repeatedly administered varying doses of DNSP-11 intranasally for 3 weeks exhibited a significant increase in dopamine (DA) turnover in both the striatum and substantia nigra (SN) at 300μg, suggestive of a stimulative effect of the dopaminergic system. Additionally, a protective effect was observed following repeated intranasal administration in 6-OHDA lesioned rats, as suggested by: a significant decrease in d-amphetamine-induced rotation at 2 weeks; a decrease in DA turnover in the lesioned striatum; and an increased sparing of tyrosine hydroxylase (TH) positive (+) neurons in a specific sub-region of the lesioned substantia nigra pars compacta (SNpc). Finally, tracer studies showed (125)I-DNSP-11 distributed diffusely throughout the brain, including the striatum and SN, as quickly as 30min after a single intranasal dose.

Comparison with existing methods: The results of bilateral intranasal administration of DNSP-11 are compared to our unilateral single infusion studies to the brain in rats.

Conclusions: These studies support that DNSP-11 can be delivered intranasally and maintain its neuroactive properties in both normal rats and in a unilateral 6-OHDA rat model of PD.

Keywords: 6-Hydroxydopamine; Intranasal administration; Neurochemistry; Neuroprotection; Nigrostriatal pathway; Peptide.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Intranasal
  • Analysis of Variance
  • Animals
  • Antiparkinson Agents / pharmacokinetics
  • Antiparkinson Agents / therapeutic use*
  • Autoradiography
  • Corpus Striatum / drug effects
  • Corpus Striatum / metabolism
  • Dextroamphetamine / pharmacology
  • Disease Models, Animal
  • Dopamine / metabolism
  • Dose-Response Relationship, Drug
  • Functional Laterality / drug effects
  • Male
  • Oligopeptides / pharmacokinetics
  • Oligopeptides / therapeutic use*
  • Oxidopamine / toxicity
  • Parkinson Disease / drug therapy*
  • Parkinson Disease / etiology
  • Parkinson Disease / pathology
  • Rats
  • Rats, Inbred F344
  • Substantia Nigra / drug effects
  • Substantia Nigra / metabolism
  • Time Factors
  • Tyrosine 3-Monooxygenase / metabolism

Substances

  • Antiparkinson Agents
  • Oligopeptides
  • prolyl-prolyl-glutamyl-alanyl-prolyl-alanyl-glutamyl-aspartyl-arginyl-seryl-leucinamide
  • Oxidopamine
  • Tyrosine 3-Monooxygenase
  • Dextroamphetamine
  • Dopamine