Brain targeting efficiency of antimigrain drug loaded mucoadhesive intranasal nanoemulsion
Abstract
Zolmitriptan (ZT) is a well-tolerated drug in migraine treatment suffering from low bioavailability due to low amount of the drug that reaches the brain after oral and nasal delivery. Development of new nasal mucoadhesive nanoemulsion formulation for zolmitriptan may success in delivering the drug directly from the nose to the brain to achieve rapid onset of action and high drug concentration in the brain which is required for treatment of acute migraine. ZT mucoadhesive nanoemulsion were prepared and characterized for drug content, zeta potential, particle size, morphology, residence time and permeation through the nasal mucosa. The selected formula was tested in-vivo in mice for its pharmacokinetics in comparison with intravenous and nasal solution of zolmitriptan. Results showed that addition of chitosan as mucoadhesive agent in 0.3% concentration to the nanoemulsion enhanced its residence time and zetapotential with no significant effect on the globule size. All tested formulations showed higher permeability coefficients than the zolmitriptan solution through the nasal mucosa. In-vivo studies showed that the mucoadhesive nanoemulsion formulation of zolmitriptan has higher AUC 0-8 and shorter T max in the brain than the intravenous or the nasal solution. This was related to the small globule size and higher permeability of the formulation.
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Important differences exist between classical macroemulsions, nanoemulsions and microemulsions in droplet size range and stability characteristics.
“Important differences can be found between classical macroemulsions (classical emulsions), NEs and microemulsions in droplet size range and stability characteristics [32,47].”
From Nanoemulsions for “Nose-to-Brain” Drug Delivery (2019) · cites this paper as [47]
In Sprague-Dawley rats, mucoadhesive chitosan-containing zolmitriptan nanoemulsion presents higher AUC and shorter Tmax in the brain than intravenous or nasal solutions.
“In vivo studies carried out on Sprague–Dawley rats showed that the mucoadhesive (chitosan containing) NE presents higher AUC and shorter Tmax in the brain than intravenous or the nasal solutions.”
From Nanoemulsions for “Nose-to-Brain” Drug Delivery (2019) · cites this paper as [47]
Addition of chitosan as a mucoadhesive agent at 0.3% to zolmitriptan nanoemulsions enhanced residence time and zeta potential with no relevant effect on globule size.
“The addition to the NE of chitosan as a mucoadhesive agent in 0.3% enhanced the residence time and zeta potential of the formulation with no relevant effect on the globule size.”
From Nanoemulsions for “Nose-to-Brain” Drug Delivery (2019) · cites this paper as [47]
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- Authors
- Abdou, E. M., Kandil, S. M., & Miniawy, H. M. F. E.
- Affiliations
- National Organization for Drug Control and Research (EG)
- Modern University for Information and Technology (EG)
- Cairo University (EG)
- Corresponding author
- Abdou, Ebtsam M.
- Venue
- International Journal of Pharmaceutics
- Publisher
- Elsevier BV
- Published
- 2017-08
- Volume
- 529
- Issue
- 1-2
- Pages
- 667-677
- ISSN
- 0378-5173 (ISSN-L)
- OpenAlex
- W2735486104
- Cited by
- 124
- References
- 74
- Citations by year
- 2026: 8 · 2025: 15 · 2024: 17 · 2023: 12 · 2022: 18 · 2021: 15 · 2020: 17 · 2019: 18 · 2018: 4
- FWCI
- 5.51
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- International Journal of Pharmaceutics (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Inhalation and Respiratory Drug Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
- Keywords
- zolmitriptan, migraine, intranasal drug delivery, chitosan, nasal mucosa permeation, brain targeting, pharmacokinetics, residence time, globule size, zeta potential, acute migraine treatment
- MeSH terms
- Administration, Intranasal, Animals, Brain, Chemistry, Pharmaceutical, Migraine Disorders, Nasal Mucosa, Tryptamines, Oxazolidinones, Mice
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