Development and Evaluation of an In Situ Nasal Gel Formulation of Desloratadine

The purpose of this study was to develop and optimize a nasal mucoadhesive in situ gel of desloratadine using the polymer Carbopol 940. This gel formulation offers promising potential for future applications in treating nasal conditions.

Six formulations with different concentrations of Carbopol 940 and xanthan gum were prepared using the cold method. Glycerin was used as a humectant, and triethanolamine was used to adjust the pH. In this study, gelation temperature, gelation time, mucoadhesive force, and viscosity were evaluated. The gel strength, in vitro drug release, and ex vivo permeation studies were also conducted for the gel formulations.

The optimum formulation, F3 (0.8% Carbopol 904), had gelation temperature 32.7± 0.22 °C, gelation time of 68 ± 1.4 seconds, mucoadhesive force 3900.45 ± 0.15 dyne/cm2, viscosity of 2882±0.3 cP, gel strength of 36 ± 0.23 seconds, 99% in vitro drug release in 6 hours and 65 % ex vivo permeation in 12 hours. Drug content was (97.66-98.99%) for all formulations. FTIR tests confirmed that there was no chemical interaction.

It was found that an increase in carbopol concentration increased the gel viscosity. The mucoadhesive strength for formulations containing Carbopol was higher than that of other formulations containing xanthan gum. The rapid hydration and swelling behavior of carbopol result in better drug diffusion. The developed nasal in situ gels may keep the drug in the matrix network and restrict fast drug release, preserving their integrity.

Desloratadine can be successfully formulated as an in situ nasal gel for nasal administration.