Abstract
Background Granisetron is a serotonin 5-HT3 receptor
antagonist used as an antiemetic to treat nausea and vomiting following
chemotherapy and radiotherapy. Its main effect is to reduce the activity of the
vagus nerve, which is a nerve that activates the vomiting center in the medulla
oblongata.
Objectives In this research mucoadhesive microspheres were developed in
order to carry out the absorption of drug through nasal mucosa with the aim to
improve therapeutic efficacy, avoid hepatic first pass metabolism and increase
residence time.
Material and Methods Mucoadhesive microspheres of Granisetron using
chitosan as polymer were prepared by emulsification cross-linking method to
increase the residence time on the mucosa. The surface of prepared microspheres
was characterized by SEM (Scanning electron microscopy) and evaluated for
particle size, encapsulation efficiency, production yield, swelling ability,
in-vitro mucoadhesion, in-vitro drug release and stability
study.
Result Among all the formulations F6 with drug/polymer ratio of
1:3 displayed the best result. On drug release kinetic model study, all the
formulations follow Zero order. Stability studies revealed that the microspheres
kept at 25±2°C and 60±5% RH showed the maximum
stability.
Conclusion After all the evaluation parameters and result obtained it can
be said that these results confirmed the suitability of Granisetron mucoadhesive
chitosan microspheres for nasal delivery system.
Key words
drug delivery - pharmaceutics - pharmacokinetics
