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Purpose <p>Despite the availability of nasal drops, sprays and oral tablets for the treatment of allergic rhinitis and other inflammatory nasal conditions, those traditional therapeutic options fail to maintain sufficient drug concentration at the nasal cavity due to systemic distribution or rapid mucociliary clearance which compromises the clinical outcomes. Mizolastine (MZL) a second-generation antihistamine has a potent H1 receptor antagonistic activity and mast cell stabilizing effect offering a great efficacy in treating different allergic conditions. However, MZL clinical efficacy is hindered by its suboptimal solubility and oral bioavailability.</p> Methods <p>MZL was formulated as proliposomes (PLs) and optimized for particle size, entrapment efficiency and in vitro release rate. The optimized MZL-PLs formula (particle size 182.2&#xa0;nm, 80.2% EE, and 63.52% MZL release at 12&#xa0;h) was incorporated into a dual responsive mucoadhesive polymeric system composed of Carbopol 940 (CP-940) and Pluronic F-127 (PF-127) designed to undergo sol–gel transition upon exposure to nasal physiological conditions to enhance the nasal retention, and therapeutic efficacy of MZL in allergic rhinitis and nasal inflammatory conditions.</p> Results <p>The selected in-situ gel formulation exhibited favorable mucoadhesive and rheological behavior with a higher release rate compared to pure MZL (59.63% compared to 31.19% MZL release after 12&#xa0;h.). Histopathological evaluation demonstrated marked attenuation of inflammatory cell infiltration and restoration of nasal mucosal architecture, supporting preliminary efficacy of the developed system as a promising approach for the management of allergic rhinitis and nasal inflammatory disorders with improved bioavailability and mucosal compatibility.</p> Conclusions <p>This study confirms the potential of an in-situ nasal MZL-PLs gel as an effective localized therapy of allergic rhinitis and related inflammatory nasal disorders.”</p>

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Mizolastine Proliposomes: Formulation, Characterization and Histopathological Insights in Allergic Rhinitis

  • 期刊论文

  • 发表日期：

    2026年4月30日

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  • Reham A. Abd Elkarim,
  • Dina Fathallah,
  • Hanan A. Abd Elkarim,
  • Sara A. Abouelmagd,
  • Ahmed A. El-Shenawy

摘要

Purpose

Despite the availability of nasal drops, sprays and oral tablets for the treatment of allergic rhinitis and other inflammatory nasal conditions, those traditional therapeutic options fail to maintain sufficient drug concentration at the nasal cavity due to systemic distribution or rapid mucociliary clearance which compromises the clinical outcomes. Mizolastine (MZL) a second-generation antihistamine has a potent H1 receptor antagonistic activity and mast cell stabilizing effect offering a great efficacy in treating different allergic conditions. However, MZL clinical efficacy is hindered by its suboptimal solubility and oral bioavailability.

Methods

MZL was formulated as proliposomes (PLs) and optimized for particle size, entrapment efficiency and in vitro release rate. The optimized MZL-PLs formula (particle size 182.2 nm, 80.2% EE, and 63.52% MZL release at 12 h) was incorporated into a dual responsive mucoadhesive polymeric system composed of Carbopol 940 (CP-940) and Pluronic F-127 (PF-127) designed to undergo sol–gel transition upon exposure to nasal physiological conditions to enhance the nasal retention, and therapeutic efficacy of MZL in allergic rhinitis and nasal inflammatory conditions.

Results

The selected in-situ gel formulation exhibited favorable mucoadhesive and rheological behavior with a higher release rate compared to pure MZL (59.63% compared to 31.19% MZL release after 12 h.). Histopathological evaluation demonstrated marked attenuation of inflammatory cell infiltration and restoration of nasal mucosal architecture, supporting preliminary efficacy of the developed system as a promising approach for the management of allergic rhinitis and nasal inflammatory disorders with improved bioavailability and mucosal compatibility.

Conclusions

This study confirms the potential of an in-situ nasal MZL-PLs gel as an effective localized therapy of allergic rhinitis and related inflammatory nasal disorders.”