期刊
JOURNAL OF PHARMACEUTICAL SCIENCES
卷 100, 期 4, 页码 1488-1502出版社
ELSEVIER SCIENCE INC
DOI: 10.1002/jps.22382
关键词
rokitamycin; chitosan; microspheres; nasal drug delivery; brain targeting; in vivo studies; spray drying; controlled release/delivery; site-specific delivery; CNS
资金
- MiUR [PRIN05]
- Fondazione Banco di Sardegna
Intranasal delivery is an alternative method to target therapeutics to the central nervous system. In the present study, chitosan glutamate (CG)-based mucoadhesive microspheres containing rokitamycin (RK) were prepared by spray-drying and in vitro characterization. Moreover, the influence of CG on RK absorption in bloodstream and cerebrospinal fluid (CSF) was evaluated after nasal administration to rats. The in vivo results were compared with those obtained after nasal administration of chitosan (CH)-based microparticles containing RK and after intravenous (IV) administration of the free drug. The in vitro results indicate that the concentrations of feed solution or kind of CH influence the RK entrapment and size of microspheres. All formulations increase the solubility of this poorly water-soluble drug, but CG is more able to increase the in vitro dissolution rate of RK than CH. CG microspheres absorb water quickly and then dissolve, whereas CH particles need more volume of water for swelling and gelling. In vivo studies showed that, after IV administration, RK is not able to cross the blood-brain barrier and to reach the CSF from the bloodstream. On the contrary, drug goes to the CSF and the bloodstream only after nasal administration of CG microparticles. (c) 2010 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:1488-1502, 2011
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