Ondansetron loaded pectin based microspheres for nasal administration: In vitro and in vivo studies

The aim of this study was the production of ondansetron hydrochloride loaded polymeric microspheres for delivery via the nasal route with aim to avoid hepatic first-pass metabolism, and enhance residence time. The microspheres were prepared by the spray–drying technique using pectin as the polymer. The objective of this study was to examine extensively the influence of formulation and process variables on the characteristics of the microspheres prepared. The effects of various experimental parameters such as drug to polymer concentration and liquid feed flow rate on particle size and entrapment efficiency were evaluated by means of experimental factorial designs. A 32 full factorial design was employed in formulating the microspheres with polymer concentration (X1) and liquid feed flow rate (X2) as independent variables and particle size and entrapment efficiency were dependent variables. The results showed that the X1X2 interaction had effect on particle size where as X2 alone effect on entrapment efficiency. The optimal microspheres were evaluated with respect to zeta potential study, drug release kinetic study, ex vivo permeation study, histological examination, stability study and in vivo study. Microspheres were characterized by differential scanning calorimetry, scanning electron microscopy and X-ray diffraction study. Scanning electron microscopy confirmed the smooth spherical surface of microspheres where as kinetic model revealed that drug release followed case II transport. The nasal delivery showed increased bioavailability as compared to oral delivery. In conclusion, the pectin containing microspheres of ondansetron hydrochloride with mucoadhesive property are suitable for nasal delivery.

In this study spray dried microspheres based on pectin for intranasal administration of ondansetron were prepared. The microspheres found to be spherical with size ranges from 11–13 µm. Microspheres had sufficient mucoadhesive strength for prolonged retention. Histological examination assures safety of formulation. In vivo study revealed significant improvement in bioavailability of ondansetron due to avoidance of first pass metabolism.Figure optionsDownload as PowerPoint slideHighlights
► We prepare mucoadhesive microspheres using pectin for nasal delivery.
► Mucoadhesion is significant for increase in residence time of drug in nasal cavity.
► Spray drying is suitable technique for preparation of uniform size microspheres.
► Microsphere formulation found to safe to nasal mucosa and results in improvement in bioavailability of ondansetron.