Montelukast nasal spray: formulation development and in vitro evaluation.

OBJECTIVES: The aim of this study was to evaluate potential development of montelukast sodium (MTS) as a nasal spray. MATERIALS AND METHODS: The formulations were prepared using hydroxypropyl cellulose (HPC) and carbomer 940 (C940). The prepared formulations were evaluated for clarity, pH, hydrodynamic size, zeta potential, viscosity, contact angle, surface tension, droplet size distribution, muco-adhesiveness, drug release, and stability. The suitable formulations were also assessed for their effects on nasal epithelial cells. RESULTS AND DISCUSSION: At room temperature (25 °C), the formulation containing 0.01% w/v C940 exhibited suitable viscosity and rheological properties. Spray droplets were in ranges of 10-40 µm, which are suitable for nasal administration. The works of adhesion of the formulations containing HPC or C940 were in the range of 0.8-4.0 and 0.2-27 µJ, respectively. In addition, the formulation containing 0.01% w/v C940 and the 0.5-15 µg/50 µL concentrations of MTS showed no signs of cytotoxicity and did not open the tight junction of nasal epithelial cells. CONCLUSION: The formulated MTS nasal spray is ideal for nasal administration for the treatment of allergic rhinitis. The formulation containing 0.01% w/v C940 had no toxicity nor alteration on the tight junction of nasal epithelial cells.