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Influence of polymeric microcarriers on the in-vivo intranasal uptake of an anti-migraine drug for brain targeting
Department of Chemistry and Pharmacy, University of Sassari.
Department of Chemistry and Pharmacy, University of Sassari.
Department of Experimental and Clinical Medicine, Pharmacology Section, University of Ferrara.
Department of Experimental and Clinical Medicine, Pharmacology Section, University of Ferrara.
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2013 (English)In: European journal of pharmaceutics and biopharmaceutics, ISSN 0939-6411, E-ISSN 1873-3441, Vol. 83, no 2, p. 174-183Article in journal (Refereed) Published
Abstract [en]

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 8 h 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 of 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 1 h.

Place, publisher, year, edition, pages
2013. Vol. 83, no 2, p. 174-183
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Other Health Sciences
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Health Science
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URN: urn:nbn:se:ltu:diva-11190DOI: 10.1016/j.ejpb.2012.10.010ISI: 000316041400007PubMedID: 23153670Scopus ID: 2-s2.0-84873710809Local ID: a18a9960-938f-42d6-928c-556747dcf2d7OAI: oai:DiVA.org:ltu-11190DiVA, id: diva2:984139
Note
Validerad; 2013; 20121113 (andbra)Available from: 2016-09-29 Created: 2016-09-29 Last updated: 2018-07-10Bibliographically approved

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Alhalaweh, AmjadVelaga, Sitaram

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