Design and Evaluation of Buccoadhesive Microspheres for Smoking Cessation

The present research work was designed with an aim to develop and evaluate buccoadhesive microspheres by cross linking method and determine the suitability of the formulation in nicotine replacement therapy. The developed microspheres were evaluated for various physicochemical parameters like appearance, particle size distribution, DSC studies, angle of repose, drug content, mucoadhesion time, in vitro release behaviour and ex vivo drug permeation through porcine buccal mucosa. The release kinetics was further explored by using Korsmeyer- Peppas equation. Stability studies of optimized batches of microspheres were carried out as per ICH guidelines. The optimized batch was found to have the particle size between 100- 150 μm and angle of repose 28.34±0.2, thus showing good flowability. The DSC thermogram revealed the engulfment of the drug into microspheres. The drug content of all the batches was found to be in the range of 96-105%. The mucoadhesion time was found to be 8.4±0.5 hrs. The in vitro release profile revealed that the drug release was sustained for 8hrs. The n value nearer to 0.5 indicates that the drug followed the Fickian diffusion pattern of release kinetics. Further ex vivo permeation studies of microspheres showed 88.91% drug permeation through the buccal mucosa in 8 hours with good correlation coefficient 0.9980 with the in vitro dissolution studies. Thus the developed microspheres will be a very effective buccal drug delivery system for the treatment of nicotine addiction.