Chitosan microspheres as a delivery system for nasal insufflation

Abstract

The aim of the present study was to develop and characterize chitosan mucoadhesive microspheres for nasal delivery. The microspheres were prepared by emulsification-crosslinking method and evaluated for morphology, particle size, swelling index, in vitro mucoadhesion and delivery properties from Miat(®) nasal insufflator. The results showed that the microspheres were spherical in shape with smooth surfaces. The particle size of microspheres was found to be dependent on the concentration of the chitosan. The mean particle size was significantly increased when high concentration of chitosan was used. Aqueous to oil phase ratio, stirring rate and dioctyl sodium sulfosuccinate (DOSS) concentration also influenced the particle size distribution of the microspheres. It was found that, as stirring rate was increased, the size of the microspheres was decreased. The volume of glutaraldehyde and crosslinking time had very slight effect on particle size distribution. The % equilibrium water uptake of the microspheres was ranged from 124% to 232% and the mucoadhesive strength from 70.64±2.14 to 86.32±3.96%. The results of powder delivery from the device showed that, almost entire amount was delivered after three puffs. The images of the delivery sequences of microsphere powder clouds demonstrated that microspheres were delivered forming an elongated puff. The core of the clouds was homogeneous which can be expected to provide effective distribution pattern.