Mucoadhesive Microspheres of Ondansetron Hydrochloride for Nasal Delivery

H.S. Mahajan, S.G. Gattani, S.J. Surana

Abstracts: Systemic delivery of drugs via nasal route has many advantages for protein and peptide drug molecules as well as conventional molecules. Mucoadhesive drug delivery systems are those that provide intimate contact of the drug with the mucosa for an extended period of time. In present work chitosan mucoadhesive microspheres of ondansetron HCL were prepared by spray-drying method, with an aim to avoid first pass effect and to improve therapeutic efficacy of Ondansetron in treatment of nausea and vomiting. Preformulation studies were carried out in order to find out the drug excipient interaction. Formulations were evaluated for physical characteristics such as particle size, incorporation efficiency, swelling ability in vitro bioadhesion and in vitro drug release in pH 6.6 phosphate buffer.Chitosan microspheres showed very good mucoadhesion due to electrostatic attraction between chitosan and mucin. The release of ondansetron hydrochloride from these microspheres was fast. These in vitro results show that spray-dried microspheres based on chitosan could be suitable nasal mucoadhesive delivery system for administration of ondansetron hydrochloride.

Although nasal administration of drug has many advantages, it is usually limited by the specific nasal morphological and physiological characteristics. One of the most important disadvantages is nasal mucociliary clearance that limits the time allowed for drug absorption to occur. Thus, mucoadhesive microspheres have been developed in order to decrease the effect of mucociliary clearance. Microspheres also exert a direct effect on the mucosa resulting in the opening of tight junctions between the epithelial cells. The most commonly investigated techniques to prepare mucoadhesive microspheres have been emulsion solvent evaporation techniques. Spray drying is an alternative process that is cheaper and faster than above techniques to prepare nasal particles from mucoadhesive polymers.

Chitosan is a cationic biodegradable and biocompatible polysaccharide, which confers bioadhesive properties to microspheres due to its hydrophilicty. It is a polymer of choice, because it enhances the nasal absorption of low molecular weight molecules as well as peptides and proteins.


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