The purpose of the present work was to develop a mucoadhesive thermoreversible nasal gel with a tailored gelling temperature to provide the prolonged contact between mometasone furoate and the nasal mucosa and in order to prevent drainage of the formulation. For this purpose, in situ gel containing a thermogelling polymer poloxamer 407 (Pluronic® F-127) and a mucoadhesive polymer Carbopol® 974P NF was prepared. In this content, formulations were designed to have gelation temperature below 34°C to obtain gelation at intranasal cavity. Evaluation of the prepared in situ gels was carried out by the determination of sol-gel transition temperature, rheological and mechanical characteristics, mucoadhesion strength, drug content, physicochemical stability, in vitro release profiles, and ex vivo permeation across sheep nasal mucosa of formulations. Consequently, the in situ gel (CP5) which had favorable gelation temperature (30.1 ± 0.24°C), rheological and mechanical characteristics, in vitro release profile (T%100 180 min), and mucoadhesion strength (0.289 ± 0.0069 mJ) was developed. Consequently, the in situ gel system has been concluded as a promising approach in order to improve the therapeutic effects of intranasal mometasone furoate administration.
Background Mometasone furoate, one of the second generation intranasal corticosteroids, is currently used in suspension form due to its poor solubility. However, this is not favorable for nasal application because of the rapid elimination of the instilled drug from the nasal cavity by mucociliary clearance and delayed onset of action due to the slow dissolution of drug in suspension. Objective The aim of this study was to determine the antiallergic effects of mucoadhesive thermosensitive in situ gel containing mometasone furoate that we developed previously to prolong the contact between the drug and nasal mucosa and to prevent drainage of the formulation in an ovalbumin-induced rat model of allergic rhinitis. Methods An experimental allergic rhinitis model was developed in female Wistar albino rats by intraperitoneal injection of ovalbumin every 2 days for 14 days followed by its repeated intranasal instillation for 7 consecutive days. Intranasal instillation of ovalbumin was continued every other day for 14 days. Mometasone furoate in situ gel (5 μg/10 µl), mometasone furoate suspension (5 μg/10 µl), and physiological saline (10 µl) were administered into the bilateral nasal cavities from day 22 to day 35. Antiallergic effects were evaluated through histopathological evaluation, analysis of ovalbumin-specific serum immunoglobulin E, and a symptom score. Results Mometasone furoate in situ gel significantly decreased the nasal symptoms and ovalbumin-specific serum immunoglobulin E level as compared with mometasone furoate suspension and physiological saline. Additionally, inflammatory histological symptoms such as mucosal edema, vascular dilatation, eosinophil infiltration, and loss of cilia within the nasal mucosa of allergic rhinitis model rats were remarkably improved with the treatment of mometasone furoate in situ gel. Conclusion These results suggest that mometasone furoate in situ gel has a better therapeutic potential for the treatment of allergic rhinitis compared to mometasone furoate suspension.
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