Background: Nasal inserts are novel, solid, bioadhesive dosage forms administered via nasal
route for prolonged systemic drug delivery. The principle of the dosage form is that, after administration
nasal inserts imbibe nasal fluid from the mucosa and form a gel in the nasal cavity in order to avoid foreign
body sensation. The objective of this investigation was the development of chitosan/xanthan gum
based bioadhesive nasal inserts of antimigraine drug.
Methods: Lyophilization is more usual technique for the preparation of nasal inserts and it is one of the
applied methods for drying of solids either in the form of aqueous solution or rarely in the form of aqueous
suspension by using freeze dryers. The recent patents on Biocompatible polymer
(US20140301972A1), High molecular weight polymers (US20050048121A1), Migraine treatment
(WO2009080764A3) helped in selecting the drug and polymers. A 32 factorial design was used to investigate
the combined effect of two independent variables such as concentration of Xanthan gum (X1) and
the concentration of Chitosan (X2), onto the water uptake, bioadhesion potential and drug release which
were the dependent variables. Nine batches of the nasal inserts were developed and evaluated for water
uptake at three different pH, bioadhesion potential and drug release. The optimized nasal inserts batch
was also characterized by DSC, PXRD and SEM.
Results: The results showed that the water uptake ability of nasal insert was strongly influenced by pH of
the medium and by polycation/polyanion concentration. This investigation verifies the formation of complexes
between chitosan and xanthan gum and confirms the potential of these complexes, in achieving the
sustained antimigraine drug delivery in the nasal cavity.
Conclusion: The best nasal inserts formulation containing chitosan and xanthan gum in the ratio 0.5:0.5,
showed desirable % drug release as well as bioadhesion which may result in an increase in the nasal residence