Ondansetron-loaded chitosan microspheres for nasal antiemetic drug delivery: an alternative approach to oral and parenteral routes.
BACKGROUND
The aim of this study was to develop chitosan microspheres for nasal delivery of ondansetron hydrochloride (OND).


METHODS
Microspheres were prepared with spray-drying method using glutaraldehyde as the crosslinking agent. Microspheres were characterized in terms of morphology, particle size, zeta potential, production yield, drug content, encapsulation efficiency, and in vitro drug release.


RESULTS
All microspheres were spherical in shape with smooth surface and positively charged. Microspheres had also high encapsulation efficiency and the suitable particle size for nasal administration. In vitro studies indicated that all crosslinked microspheres had a significant burst effect, and sustained drug release pattern was observed until 24 hours following burst drug release. Nasal absorption of OND from crosslinked chitosan microspheres was evaluated in rats, and pharmacokinetic parameters of OND calculated from nasal microsphere administration were compared with those of both nasal and parenteral administration of aqueous solutions of OND. In vivo data also supported that OND-loaded microspheres were also able to attain a sustained plasma profile and significantly larger area under the curve values with respect to nasal aqueous solution of OND.


CONCLUSIONS
Based on in vitro and in vivo data, it could be concluded that crosslinked chitosan microspheres are considered as a nasal delivery system of OND.
Department of Pharmaceutical Technology, Faculty of Pharmacy, Istanbul University, Istanbul, Turkey. sgungor@istanbul.edu.tr
Sevgi
S
Gungor
Alper
A
Okyar
Sidika
S
Erturk-Toker
Gul
G
Baktir
Yildiz
Y
Ozsoy
D000281:Administration, Intranasal; D000818:Animals; D000932:Antiemetics / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics; D001682:Biological Availability; D048271:Chitosan / Q000737:chemistry*; D004337:Drug Carriers; D004339:Drug Compounding; D016503:Drug Delivery Systems; D005260:Female; D008297:Male; D008863:Microspheres; D017294:Ondansetron / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D013678:Technology, Pharmaceutical
D000932:Antiemetics; D004337:Drug Carriers; D017294:Ondansetron; D048271:Chitosan