The adenosine derivative N6-cyclopentyladenosine (CPA) has been proposed as a potent antiischemic drug for the central nervous system (CNS). Recently, the nasal route has been proposed as a promising way to target into the brain the drugs unable to overcome the physiologic barriers between blood and CNS. We report a study regarding the preparation of powder formulations containing CPA for nasal delivery. The powders have been obtained by spray-drying in the presence either of mannitol and lecithin, or chitosan as carriers. The powders have been investigated for particle size, morphology, in vitro drug release, mucoadhesive properties and drug permeation through sheep nasal mucosa. Finally, the powders have been administered in vivo to rats using Monopowder P® nasal insufflators, in order to evaluate the amounts of CPA able to reach the blood, the liquor and brain sections at different times after the administration.
Brain Targeting of an Antiischemic Agent by Nasal Administration of Microparticles
DALPIAZ, Alessandro;COLOMBO, Gaia;BORTOLOTTI, Fabrizio;FERRARO, Luca Nicola;TANGANELLI, Sergio;SCATTURIN, Angelo;MENEGATTI, Enea;
2005
Abstract
The adenosine derivative N6-cyclopentyladenosine (CPA) has been proposed as a potent antiischemic drug for the central nervous system (CNS). Recently, the nasal route has been proposed as a promising way to target into the brain the drugs unable to overcome the physiologic barriers between blood and CNS. We report a study regarding the preparation of powder formulations containing CPA for nasal delivery. The powders have been obtained by spray-drying in the presence either of mannitol and lecithin, or chitosan as carriers. The powders have been investigated for particle size, morphology, in vitro drug release, mucoadhesive properties and drug permeation through sheep nasal mucosa. Finally, the powders have been administered in vivo to rats using Monopowder P® nasal insufflators, in order to evaluate the amounts of CPA able to reach the blood, the liquor and brain sections at different times after the administration.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
