titoli, abstracts, parole chiave >>>
Influence of polymeric microcarriers on the in vivo intranasal uptake of an anti-migraine drug for brain targeting

Gavini, Elisabetta and Rassu, Giovanna and Ferraro, Luca and Beggiato, Sarah and Alhalaweh, Amjad and Velaga, Sitaram and Marchetti, Nicola and Bandiera, Pasquale and Giunchedi, Paolo and Dalpiaz, Alessandro (2013) Influence of polymeric microcarriers on the in vivo intranasal uptake of an anti-migraine drug for brain targeting. European Journal of Pharmaceutics and Biopharmaceutics, Vol. 83 (2), p. 174-183. ISSN 0939-6411. eISSN 1873-3441. Article.

Full text not available from this repository.

DOI: 10.1016/j.ejpb.2012.10.010

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 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 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 1 h.

Item Type:Article
ID Code:8584
Status:Published
Refereed:Yes
Uncontrolled Keywords:Microspheres, zolmitriptan, chitosan, nasal administration, brain targeting, in vivo studies
Subjects:Area 03 - Scienze chimiche > CHIM/09 Farmaceutico tecnologico applicativo
Area 05 - Scienze biologiche > BIO/16 Anatomia umana
Divisions:001 Università di Sassari > 01-a Nuovi Dipartimenti dal 2012 > Scienze Biomediche
001 Università di Sassari > 01-a Nuovi Dipartimenti dal 2012 > Chimica e Farmacia
Publisher:Elsevier
ISSN:0939-6411
eISSN:1873-3441
Copyright Holders:© 2012 Elsevier
Deposited On:01 Feb 2013 10:32

I documenti depositati in UnissResearch sono protetti dalle leggi che regolano il diritto d'autore

Repository Staff Only: item control page