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Background <p>Bilastine is a second-generation antihistamine used in allergic rhinitis; however, its clinical performance may be limited by poor aqueous solubility and low oral bioavailability. The present study aimed to develop and optimize a bilastine-loaded nanoemulsion as a prospective intranasal delivery system.</p> Methods <p>Bilastine nanoemulsions were developed using Capryol 90 as oil phase, Cremophor EL as surfactant, and PEG 400 as co-surfactant. Pseudo-ternary phase diagrams and thermodynamic stability studies were used for formulation screening. A Box-Behnken design evaluated the influence of oil concentration, Smix concentration, and stirring speed on globule size, polydispersity index (PDI), and zeta potential. The optimized formulation was characterized for globule size, PDI, zeta potential, morphology by TEM, pH, in vitro release, ex vivo permeation across goat nasal mucosa, and confocal laser scanning microscopy (CLSM).</p> Results <p>The optimized nanoemulsion exhibited a globule size of 129.1 ± 5.97&#xa0;nm, PDI of 0.214 ± 0.045, zeta potential of + 8.405 ± 0.241 mV, and spherical morphology on TEM. The formulation showed higher in vitro drug release over 24&#xa0;h (82.74 ± 5.78%) than the conventional formulation (49.91 ± 3.48%). In the ex-vivo study, cumulative permeation at 8&#xa0;h was 0.225 ± 0.018&#xa0;mg/cm² for the nanoemulsion versus 0.165 ± 0.014&#xa0;mg/cm² for the conventional formulation (<i>p</i> = 0.0119), with an estimated flux of 0.0209 and 0.0162&#xa0;mg/cm²/h, respectively. CLSM demonstrated deeper penetration of the nanoemulsion across goat nasal mucosa (approximately 35&#xa0;μm) than the conventional formulation (approximately 15&#xa0;μm).</p> Conclusion <p>The optimized bilastine-loaded nanoemulsion showed favorable physicochemical properties, improved release, enhanced ex-vivo permeation, and deeper mucosal penetration compared with the conventional formulation. These findings support its potential as a promising intranasal delivery platform for bilastine, while further spray-performance, long-term stability, and in vivo studies are warranted.</p>

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Development and Evaluation of a Bilastine-Loaded Nanoemulsion for Intranasal Delivery in Allergic Rhinitis

  • 期刊论文

  • 发表日期：

    2026年4月14日

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  • Keshav Kumar,
  • Rupali Sharma,
  • Satish Sardana

摘要

Background

Bilastine is a second-generation antihistamine used in allergic rhinitis; however, its clinical performance may be limited by poor aqueous solubility and low oral bioavailability. The present study aimed to develop and optimize a bilastine-loaded nanoemulsion as a prospective intranasal delivery system.

Methods

Bilastine nanoemulsions were developed using Capryol 90 as oil phase, Cremophor EL as surfactant, and PEG 400 as co-surfactant. Pseudo-ternary phase diagrams and thermodynamic stability studies were used for formulation screening. A Box-Behnken design evaluated the influence of oil concentration, Smix concentration, and stirring speed on globule size, polydispersity index (PDI), and zeta potential. The optimized formulation was characterized for globule size, PDI, zeta potential, morphology by TEM, pH, in vitro release, ex vivo permeation across goat nasal mucosa, and confocal laser scanning microscopy (CLSM).

Results

The optimized nanoemulsion exhibited a globule size of 129.1 ± 5.97 nm, PDI of 0.214 ± 0.045, zeta potential of + 8.405 ± 0.241 mV, and spherical morphology on TEM. The formulation showed higher in vitro drug release over 24 h (82.74 ± 5.78%) than the conventional formulation (49.91 ± 3.48%). In the ex-vivo study, cumulative permeation at 8 h was 0.225 ± 0.018 mg/cm² for the nanoemulsion versus 0.165 ± 0.014 mg/cm² for the conventional formulation (p = 0.0119), with an estimated flux of 0.0209 and 0.0162 mg/cm²/h, respectively. CLSM demonstrated deeper penetration of the nanoemulsion across goat nasal mucosa (approximately 35 μm) than the conventional formulation (approximately 15 μm).

Conclusion

The optimized bilastine-loaded nanoemulsion showed favorable physicochemical properties, improved release, enhanced ex-vivo permeation, and deeper mucosal penetration compared with the conventional formulation. These findings support its potential as a promising intranasal delivery platform for bilastine, while further spray-performance, long-term stability, and in vivo studies are warranted.