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Brain uptake of an anti-ischemic agent by nasal administration of microparticles

Dalpiaz, Alessandro and Gavini, Elisabetta and Colombo, Gaia and Russo, Paola and Bortolotti, Fabrizio and Ferraro, Luca and Tanganelli, Sergio and Scatturin, Angelo and Menegatti, Enea and Giunchedi, Paolo (2008) Brain uptake of an anti-ischemic agent by nasal administration of microparticles. Journal of Pharmaceutical Sciences, Vol. 97 (11), p. 4889-4903. eISSN 1520-6017. Article.

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DOI: 10.1002/jps.21335


N6-cyclopentyladenosine (CPA) has neuronal anti-ischemic properties, but it is not absorbed into the brain from the bloodstream, where it shows poor stability and induces side effects. Microparticulate drug delivery systems designed for CPA nasal administration and constituted by mannitol or chitosan, were prepared by spray-drying and characterized. Mannitol-lecithin microparticles showed high CPA dissolution rate, whereas chitosan microparticles controlled its release rate. In vitro mucoadhesion studies indicated that CPA-loaded chitosan microparticles had higher mucoadhesive properties compared to mannitol particles. Ex vivo studies on sheep nasal mucosa showed that mannitol microparticles promoted CPA permeation across the mucosa, whereas chitosan microparticles controlled CPA permeation rate in comparison with CPA raw material. In vivo studies were carried out on rats. No CPA was detected in rat cerebrospinal fluid (CSF) and brain sections after intravenous administration. In contrast, after nasal administration of loaded microparticles CPA was found in the CSF at concentrations ranging from high nM to µM values and up to two order of magnitude higher than those obtained at systemic level. CPA was also found in the olfactory bulb at concentrations around 0.1 ng/mg of tissue. These results can open new perspectives for the employment of CPA against brain damages following stroke.

Item Type:Article
ID Code:1774
Uncontrolled Keywords:Cerebrospinal fluid, chitosan, CNS, controlled release, drug targeting, microparticles, nasal absorption, polymeric drug carrier, spray drying
Subjects:Area 03 - Scienze chimiche > CHIM/09 Farmaceutico tecnologico applicativo
Divisions:001 Università di Sassari > 01 Dipartimenti > Scienze del farmaco
Additional Information:Pubblicato online il 25 febbraio 2008.
Deposited On:18 Aug 2009 10:06

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