Assessment Of Spanlastic Vesicles Of Zolmitriptan For Treating Migraine In Rats

Drug Des Devel Ther. 2019 Nov 21:13:3929-3937. doi: 10.2147/DDDT.S220473. eCollection 2019.

Abstract

Objective: To develop and evaluate zolmitriptan spanlastics (Zol SLs) as a brain-targeted antimigraine delivery system. Spanlastics (SLs) prepared using span 60: tween 80 (70:30%, respectively) gave the highest percentage of entrapment efficiency (EE%).

Materials and methods: A total of 60 adult male Wistar albino rats were divided into six groups (n=10 rats/group). Group 1 (Control) comprised rats serving as a negative control. Group 2 was treated with glyceryl trinitrate (NTG) and served as the positive control. Groups 3 (NTG+Zol com), Group 4 (NTG+Zol sol) and Group 5 (NTG+Zol SLs) received commercial zolmitriptan orally, zolmitriptan solution intranasally and Zol SLs F5 intranasally, respectively, 30 min before NTG. Group 6 (Zol SLs) comprised normal rats that received only Zol SLs intranasally.

Results: We found decreased Tmax, increased Cmax, AUC0-6, AUC0-∞ and ameliorated behaviour in rats (head scratching) treated with intranasal SLs compared to oral commercial zolmitriptan.

Conclusion: Our study substantiates the enhanced efficacy of Zol SLs in brain targeting for migraine treatment.

Keywords: SLs; Zol; brain targeting; intranasal delivery; migraine; pharmacodynamics; pharmacokinetics; spanlastics; zolmitriptan.

MeSH terms

  • Administration, Intranasal
  • Animals
  • Injections, Intraperitoneal
  • Male
  • Migraine Disorders / chemically induced
  • Migraine Disorders / drug therapy*
  • Nitroglycerin / administration & dosage
  • Oxazolidinones / administration & dosage
  • Oxazolidinones / blood
  • Oxazolidinones / therapeutic use*
  • Rats
  • Rats, Wistar
  • Serotonin 5-HT1 Receptor Agonists / administration & dosage
  • Serotonin 5-HT1 Receptor Agonists / blood
  • Serotonin 5-HT1 Receptor Agonists / therapeutic use*
  • Tryptamines / administration & dosage
  • Tryptamines / blood
  • Tryptamines / therapeutic use*

Substances

  • Oxazolidinones
  • Serotonin 5-HT1 Receptor Agonists
  • Tryptamines
  • zolmitriptan
  • Nitroglycerin