Formulation development of buccal tablets containing mucoadhesive nicotine microcapsules

Abstract

The present study aim to develop and evaluate buccal tablets containing mucoadhesive nicotine microcapsules. The mucoadhesive nicotine microcapsules were prepared by bottom spray fluidized-bed coater. HPMC E15 was used as the mucoadhesive polymer by varying the amount in the coating solution. Coating solution of 5% weight gain of HPMC E15 resulted in the most desirable mucoadhesive behavior. Although, the amounts of HPMC E15 were increased to more than 5% weight gain, it could not further extend the mucoadhesion time. Solid state characterization of nicotine hydrogen tartrate dihydrate (NHT) in mucoadhesive nicotine microcapsules was carried out by solid state ¹³C nuclear magnetic resonance and revealed that the addition of additives and the fluidized-bed coating process did not affect the solid state modification of NHT within the mucoadhesive nicotine microcapsules. Buccal tablets containing mucoadhesive nicotine microcapsules were prepared as a bilayer tablet by direct compression. Optimum formulation of nicotine-containing layer consisted of mucoadhesive nicotine microapsules 140 mg, D-granules 510 mg, sucralose 1 mg, menthol 12 mg, magnesium stearate 0.5% and talcum 2%. Various physicochemical evaluation of optimal formulation showed satisfactory results as seen from weight variation (0.08±0.56%), thickness (5.59±0.01mm), hardness (12.95±0.68 kg/cm2) and friability (0.14%). Tablets were evaluated for in vitro release of nicotine using modified Franz diffusion cells which illustrates a maximum nicotine release of 61.38% after 6 hours. The release rate followed zero-order rate kinetics.