Effects of a Thermosensitive In Situ Gel Containing Mometasone Furoate on a Rat Allergic Rhinitis Model

Abstract

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.

In vivo visualization and analysis of ciliary motion in allergic rhinitis models induced by ovalbumin

“…One possible reason is the destruction of the ciliary structure, including ciliary adhesion and loss, from the effect of AR. 23,24 However, the results of some experiments 16 in vitro were just the opposite; CBF increased in the mouse model of AR, which indicated that other mechanisms might also control CBF in the phase of AR. A reason for that could be the in vitro state of ciliary motion is likely to change when the original mucus on the surface of the airway was replaced by buffer solution or culture solution.…”

“…One possible reason is the destruction of the ciliary structure, including ciliary adhesion and loss, from the effect of AR. 23,24…”

A thermoresponsive hydrogel system for long-acting corticosteroid delivery into the paranasal sinuses

“…Others have designed a thermoresponsive and bioadhesive gel for 4 h of mometasone release [21]. This gel was composed of Pluronic® F-127 and Carbopol® 974P NF and tested for relieving allergic rhinitis in rats and promoting repair of a mucosal injury in rabbits [21][22][23]. Another mucoadhesive in situ gel designed for the nasal and sinus cavities was synthesized from poloxamer-407, hydroxypropyl methyl cellulose, and chitosan salt and demonstrated the gradual release of steroid, dexamethasone 21-phosphate disodium, for 3 days in vitro [24].…”

Hydrogel‐Based Intranasal Delivery Systems for The Treatment of Allergic Rhinitis

“…Thermosensitive in situ hydrogel Loratadine Ex vivo (sheep nasal mucosa) [23] 2018 Thermosensitive in situ hydrogel Mometasone furoate In vivo (Wistar albino rats) [28] 2017 Thermosensitive in situ hydrogel Mometasone furoate Ex vivo (sheep nasal mucosa) [27] 2017 Thermosensitive in situ hydrogel Polyherbal extracts Ex vivo (sheep nasal mucosa) In vivo (Swiss mice) [26] 2015 DNA hydrogel Cryj1 vaccine In vitro (murine macrophage-like RAW264.7 cells)…”