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Purpose <p>To develop and optimize rizatriptan benzoate (RZB)-loaded ethosomes to enhance brain bioavailability and bypass first-pass metabolism, then incorporate them into a thermosensitive in-situ nasal gel for improved brain-targeted migraine therapy.</p> Methods <p>RZB-loaded ethosomes were prepared and optimized using a 3² factorial design assessing ethanol and propylene glycol effects on vesicle properties. The optimized system was characterized for size, entrapment efficiency, zeta potential, morphology (HR-TEM) and compatibility (DSC, FT-IR) with in-vitro release compared to RZB solution. Ethosomes were incorporated into a thermosensitive nasal gel (Poloxamer 407 and Carbopol 974PNF) and evaluated for gelation, pH, viscosity, permeation, mucoadhesion and safety.</p> Results <p>The optimized ethosomal formulation showed a particle size of 317.3 ± 12.2 nm, entrapment efficiency of 83.51 ± 2.82% and zeta potential of −46.05 ± 2.47 mV, indicating nanoscale stability. HR-TEM confirmed spherical, bilayered vesicles. DSC and FT-IR analyses demonstrated molecular dispersion of RZB and absence of chemical incompatibility. The ethosomal system exhibited sustained in-vitro drug release (approximately 80% over 8 hours) compared to RZB solution. The thermosensitive nasal gel showed rapid gelation (&lt;1 minute at 34 °C), pH between 6.28-6.34 and suitable viscosity (3458.68 ± 104.23 cP at 34 °C). Ex-vivo studies revealed enhanced permeation (~75% in 8 hours) and higher mucoadhesive strength (2090.65 ± 104.62 dynes/cm²) compared to conventional gel. Histopathological evaluation confirmed mucosal safety.</p> Conclusion <p>The developed ethosome-based thermosensitive nasal gel represents a stable and non-invasive platform for improved brain targeting of RZB, potentially enhancing therapeutic efficacy and patient compliance in migraine management.</p> Graphical abstract <p></p>

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Development and Optimization of Rizatriptan Benzoate-Loaded Ethosomal Thermosensitive In-Situ Nasal Gel for Brain-Targeted Migraine Therapy

  • 期刊论文

  • 发表日期：

    2026年3月2日

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  • Judy Fernandes,
  • Asma Parab,
  • Mythili Krishna,
  • Ashwin Mali,
  • Bothiraja Chellampillai

摘要

Purpose

To develop and optimize rizatriptan benzoate (RZB)-loaded ethosomes to enhance brain bioavailability and bypass first-pass metabolism, then incorporate them into a thermosensitive in-situ nasal gel for improved brain-targeted migraine therapy.

Methods

RZB-loaded ethosomes were prepared and optimized using a 3² factorial design assessing ethanol and propylene glycol effects on vesicle properties. The optimized system was characterized for size, entrapment efficiency, zeta potential, morphology (HR-TEM) and compatibility (DSC, FT-IR) with in-vitro release compared to RZB solution. Ethosomes were incorporated into a thermosensitive nasal gel (Poloxamer 407 and Carbopol 974PNF) and evaluated for gelation, pH, viscosity, permeation, mucoadhesion and safety.

Results

The optimized ethosomal formulation showed a particle size of 317.3 ± 12.2 nm, entrapment efficiency of 83.51 ± 2.82% and zeta potential of −46.05 ± 2.47 mV, indicating nanoscale stability. HR-TEM confirmed spherical, bilayered vesicles. DSC and FT-IR analyses demonstrated molecular dispersion of RZB and absence of chemical incompatibility. The ethosomal system exhibited sustained in-vitro drug release (approximately 80% over 8 hours) compared to RZB solution. The thermosensitive nasal gel showed rapid gelation (<1 minute at 34 °C), pH between 6.28-6.34 and suitable viscosity (3458.68 ± 104.23 cP at 34 °C). Ex-vivo studies revealed enhanced permeation (~75% in 8 hours) and higher mucoadhesive strength (2090.65 ± 104.62 dynes/cm²) compared to conventional gel. Histopathological evaluation confirmed mucosal safety.

Conclusion

The developed ethosome-based thermosensitive nasal gel represents a stable and non-invasive platform for improved brain targeting of RZB, potentially enhancing therapeutic efficacy and patient compliance in migraine management.

Graphical abstract