Design, characterization, and evaluation of novel mucoadhesive nasal inserts for the treatment of hypertension

Abstract

Abstract Nasal inserts are novel solid, bio-adhesive dosage forms that various methods can prepare. Nasal inserts work on the principle of nasal fluid absorption from the nasal mucosa on administration into the nasal cavity, where it forms gel, avoiding foreign body sensation. They are administered via the nasal route and help to accomplish delayed systemic drug delivery. This investigation aimed to develop lyophilized nasal inserts of diltiazem hydrochloride for the treatment of hypertension using various concentrations of xanthan gum and guar gum. The drug content, surface pH, hydrophilicity studies, water uptake studies, mucoadhesive studies, in vitro drug release studies, and ex vivo permeation studies of the drug-loaded inserts were carried out. It was further characterized and evaluated by differential scanning calorimetry, scanning electron microscopy, X-ray diffraction studies, histological investigation and stability studies. Lyophilized nasal inserts have advantages over other formulations due to their high-water uptake and mucoadhesion properties. The optimized formulation showed no significant changes in the treated nasal mucosa of the goat, and the stability of the formulation was confirmed by stability studies. The nasal insert containing xanthan gum and guar gum (1:3) is the optimized one because of its high drug content and better drug release when compared to other formulations. In conclusion, the novel nasal inserts of diltiazem hydrochloride could be a better alternative for treating hypertension.