Development of Nasal Mucoadhesive Microspheres of Granisetron: A Potential Drug

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.

Formulation and Characterization of Losartan Loaded Chitosan Microspheres: Effect of Crosslinking Agents

“…In recent times, microsphere formulations have achieved tremendous significance as oral drug delivery systems due to predictable gastric emptying, reduced local irritation and fewer toxic effects as compared to unit dosage forms which make these systems more preferable. Chitosan has been used as an ex-cipient of choice in formulating biodegradable microspheres owing to its property of modifying the drug release and also exerting mucoadhesive effect [1][2][3]. Since the matrices made of cross-linked chitosan amicably alter the release of a loaded drug, so the current study endeavored the determination of effect of diverse cross-linking agents on the release of drug loaded in chitosan microspheres.…”

Research progress in brain-targeted nasal drug delivery

“…Microspheres are a spherical drug delivery system composed of various materials, including but not limited to, albumin, gelatin, polylactides, and starches ( Rassu et al, 2018 ). Microspheres act as strong bio-adhesives and can extend the retention time of drugs in the nasal cavity to 4 h ( Pandey et al, 2020 ). In addition, they can protect drugs from enzymatic metabolism, thereby greatly enhancing their bioavailability ( Pandey et al, 2020 ).…”

Different Methods and Formulations of Drugs and Vaccines for Nasal Administration

“…Microspheres are widely used in nasal drug delivery. Microspheres that are prepared by spray drying or emulsion crosslinking with cyclodextrins or chitosan as solubilizers and absorption enhancers significantly improved the in vivo bioavailability of encapsulated drugs, which enhanced drug permeation through respiratory and olfactory epithelium through transcellular transports or paracellular transport through olfactory epithelium cells [ 89 , 90 ]. It can prolong the contact time at the site of drug absorption because the surface of the microspheres has wrinkles and can adhere to the nasal mucosal epithelial cells [ 91 ]; it is also easily degraded by enzymes, and provides continuous drug release.…”