Abstract

Migraine is one of the major symptoms of many psychiatric and mental disorders like depression and anxiety. Eletriptan Hydrobromide (EH) is a well-tolerated drug in migraine treatment, but suffers from low oral bioavailability and low brain targeting after oral delivery. New nasal mucoadhesive EH-emulsomes development could be a new means to direct the drug from the nose-to-brain to achieve rapid onset of action and high drug concentration in the brain for acute migraine treatment. Eletriptan mucoadhesive emulsomes formulations were prepared using thin-film hydration method and 23 full factorial design was adopted to study different formulation factors’ effect on the emulsomes characters. The emulsomes were characterized for entrapment efficiency (EE%), zeta potential (ZP), particle size (PS), morphology, and ex-vivo permeation through the nasal mucosa. The selected formula was evaluated in mice for its in-vivo bio-distribution in comparison with EH intranasal and intravenous solutions. Drug targeting efficacy (DTE%) and nose-to-brain direct transport percentage (DTP%) were calculated. The optimization formulation showed a nanoparticle size of 177.01 nm, EE 79.44%, and ZP = 32.12 ± 3.28 mV. In addition, in-vitro permeability studies revealed enhanced drug permeability with suitable mean residence time up to 120 ± 13 min. EH-emulsomes were stable under different storage conditions for three months. In vivo examination and pharmacokinetic drug targeting parameters revealed EH transport to the CNS after EH nanoparticle nasal administration. Histopathology study showed no ciliotoxic effect on the nasal mucosa. From the results, it can be confirmed that the emulsomes formulation of EH proved safe direct nose-to-brain transport of EH after nasal administration of EH emulsomes.

Highlights

  • Introduction distributed under the terms andMigraine is a neurologic episodic headache attack, which directly affects over one billion people across all world regions [1]

  • The results indicated that the optimized formula shows nanoparticle size 177.013 nm, size79.44%, 177.013ZP

  • These results indicated that the optimized. These results indicated that the optimized Eletriptan Hydrobromide (EH) emulsomes formula No 10 is the best best selected formula

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Summary

Introduction

Migraine is a neurologic episodic headache attack, which directly affects over one billion people across all world regions [1]. It was the major symptom of many psychiatric and mental disorders such as depression and anxiety [2,3,4]. Pharmaceutics 2022, 14, 410 suitable formulation that can give quick onset of action [5,6]. Migraine headache is due to neurogenic inflammation of the trigeminal nerve in the cranial dura mater [7]. These central stimulations can participate in trigeminal neurons sensitization and activation [8]

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