Development and Characterization of Niaprazine-Loaded Xanthan Gum-Based Gel for Oral Administration.

Niaprazine is a sedative-hypnotic drug initially developed as an antihistamine and used for its notable sedative effects, particularly in children. Following its withdrawal from the market by the producer, the drug has been administered as magistral formulations available in syrup form, but there are several important disadvantages to this, including instability, taste issues, lack of controlled release, and the potential for unreliable dosing due to incomplete swallowing. There is also an increased risk of dental caries, as well as the fact that these formulations are not suitable for children who suffer from diabetes. The purpose of the current investigation is to prepare and characterize xanthan gum-based gels for the oral administration of niaprazine. Niaprazine gels appear as transparent-whiteish, non-sticky substances, with the drug uniformly dispersed throughout the systems. They are also stable over time. Dynamic rheology revealed their advantageous shear-thinning properties, which enable the formulation to be flexibly dosed orally through administration via syringe. During experimentation, the evaluation of the mucoadhesion features and the in vitro drug release profile were also performed. The results demonstrate that the formulation may represent an alternative to niaprazine syrup, allowing easy preparation, administration, and increased compliance in various categories of patients, including pediatric.