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Background <p>Schizophrenia is a chronic neuropsychiatric disorder requiring sustained therapeutic drug levels in the brain. Oral Cariprazine HCl is limited by extensive first-pass metabolism, low bioavailability, and delayed onset of action.</p> Methods <p>A thermoresponsive, mucoadhesive intranasal in-situ gel of Cariprazine HCl was developed and optimized using a 3<sup>2</sup> Central Composite Design, with Poloxamer 407 and Carbopol 934P as independent variables. Formulations were evaluated for gelation behavior, mucoadhesion, rheological properties, drug release, and ex-vivo nasal permeation.</p> Results <p>The optimized formulation (F11) exhibited rapid sol–gel transition at physiological temperature (gelation time: 8.2 ± 0.2&#xa0;s at 34&#xa0;°C) and high mucoadhesive strength (5212.76 dyne/cm²). Sustained drug release of 97.17% was achieved over 24&#xa0;h, following diffusion-controlled kinetics. Ex-vivo permeation studies across goat nasal mucosa demonstrated significantly enhanced drug permeation (72.3% at 24&#xa0;h) compared with pure drug dispersion. ATR-FTIR confirmed drug–excipient compatibility, histopathological evaluation showed no mucosal damage, and stability studies over 90 days indicated formulation robustness.</p> Conclusion <p>The developed intranasal in-situ gel provides a non-invasive and effective platform for improving nasal retention, sustained release and intranasal delivery with potential for nose-to-brain transport of Cariprazine HCl, offering a promising alternative to conventional oral therapy for schizophrenia.</p> Graphical Abstract <p></p>

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Design, Development, and Evaluation of In-Situ Nasal Gel of an Antipsychotic Drug

  • 期刊论文

  • 发表日期：

    2026年4月1日

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  • Ayesha Syed,
  • Preeti Karwa,
  • Sohal Mallick,
  • Ankita Mohanty

摘要

Background

Schizophrenia is a chronic neuropsychiatric disorder requiring sustained therapeutic drug levels in the brain. Oral Cariprazine HCl is limited by extensive first-pass metabolism, low bioavailability, and delayed onset of action.

Methods

A thermoresponsive, mucoadhesive intranasal in-situ gel of Cariprazine HCl was developed and optimized using a 32 Central Composite Design, with Poloxamer 407 and Carbopol 934P as independent variables. Formulations were evaluated for gelation behavior, mucoadhesion, rheological properties, drug release, and ex-vivo nasal permeation.

Results

The optimized formulation (F11) exhibited rapid sol–gel transition at physiological temperature (gelation time: 8.2 ± 0.2 s at 34 °C) and high mucoadhesive strength (5212.76 dyne/cm²). Sustained drug release of 97.17% was achieved over 24 h, following diffusion-controlled kinetics. Ex-vivo permeation studies across goat nasal mucosa demonstrated significantly enhanced drug permeation (72.3% at 24 h) compared with pure drug dispersion. ATR-FTIR confirmed drug–excipient compatibility, histopathological evaluation showed no mucosal damage, and stability studies over 90 days indicated formulation robustness.

Conclusion

The developed intranasal in-situ gel provides a non-invasive and effective platform for improving nasal retention, sustained release and intranasal delivery with potential for nose-to-brain transport of Cariprazine HCl, offering a promising alternative to conventional oral therapy for schizophrenia.

Graphical Abstract