Influence of polymeric microcarriers on the in vivo intranasal uptake of an anti-migraine drug for brain targeting
Abstract
The objective of this study was to investigate the effect of polymeric microcarriers on the in vivo intranasal uptake of an anti-migraine drug for brain targeting. Mucoadhesive powder formulations consisted of antimigraine drug, zolmitriptan, and chitosans (various molecular weights and types) or hydroxypropyl methylcellulose (HPMC). Their suitability for nasal administration was evaluated by in vitro and ex vivo mucoadhesion and permeation tests. The formulations based on chitosan glutamate (CG) or HPMC were tested in vivo because they showed good mucoadhesive properties and altered the permeation rate of the drug. The in vivo results from intravenous infusion and nasal aqueous suspension of the drug or nasal particulate powders were compared. The plasmatic AUC values obtained within 8h following intravenous administration appeared about three times higher than those obtained by nasal administration, independent of the formulations. Zolmitriptan concentrations in the cerebrospinal fluid obtained from nasal and intravenous administrations were, respectively, 30 and 90 times lower than the concentrations of the drug in the blood. Thus, nasal administration potentiated the central zolmitriptan activity, allowing a reduction in the drug peripheral levels, with respect to the intravenous administration. Among nasally administered formulations, CG microparticles showed the highest efficacy in promoting the central uptake of zolmitriptan within 1h.
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Nasal administration of drugs using the nose-to-brain pathway allows direct drug targeting into the brain, avoiding the first-pass effect and bypassing the BBB.
“The nasal administration of drugs using the nose-to-brain pathway allows direct drug targeting into the brain, avoiding the first-pass effect and bypassing the BBB.”
From Nanoemulsions for “Nose-to-Brain” Drug Delivery (2019) · cites this paper as [14]
Nose-to-brain drug delivery is a painless, non-invasive administration route that can deliver therapeutic agents into the brain by bypassing the blood-brain barrier.
“Nose-to-brain drug delivery is a painless, non-invasive administration route that can be used to deliver therapeutic agents into the brain by bypassing the BBB [10,14,15,16,17].”
From Nanoemulsions for “Nose-to-Brain” Drug Delivery (2019) · cites this paper as [14]
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- Authors
- Gavini, E., Rassu, G., Ferraro, L., Beggiato, S., Alhalaweh, A., Velaga, S., Marchetti, N., Bandiera, P., Giunchedi, P., & Dalpiaz, A.
- Affiliations
- University of Sassari (IT)
- University of Ferrara (IT)
- Luleå University of Technology (SE)
- Corresponding author
- Giunchedi, Paolo
- ORCID
- Venue
- European Journal of Pharmaceutics and Biopharmaceutics
- Publisher
- Elsevier BV
- Published
- 2013-02
- Volume
- 83
- Issue
- 2
- Pages
- 174-183
- ISSN
- 0939-6411 (ISSN-L)
- OpenAlex
- W2057586244
- Cited by
- 62
- References
- 51
- Citations by year
- 2026: 2 · 2025: 2 · 2024: 4 · 2023: 6 · 2022: 6 · 2021: 5 · 2020: 7 · 2019: 3 · 2018: 5 · 2017: 5 · 2016: 3 · 2015: 8 · 2014: 5
- FWCI
- 2.58
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- European Journal of Pharmaceutics and Biopharmaceutics (publishedVersion)
- PubMed (publishedVersion)
- Institutional Research Information System University of Ferrara (University of Ferrara) (submittedVersion)
- UnissResearch (Università degli Studi di Sassari) (submittedVersion)
- Funders
- Kempe Foundation
- European Regional Development Fund
- 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
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Keywords
- zolmitriptan, intranasal drug delivery, brain targeting, hydroxypropyl methylcellulose, nasal permeation, cerebrospinal fluid drug concentration, antimigraine drugs, brain drug delivery
- MeSH terms
- Adhesives, Administration, Intranasal, Animals, Brain, Chemistry, Pharmaceutical, Drug Carriers, Migraine Disorders, Nasal Mucosa, Permeability, Polymers, Powders, Swine, Tryptamines, Glutamic Acid, Area Under Curve, Oxazolidinones, Chitosan, Administration, Intravenous, Hypromellose Derivatives
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