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2000
Volume 15, Issue 3
  • ISSN: 2468-1873
  • E-ISSN: 2468-1881

Abstract

Background

Iloperidone is a second-generation antipsychotic drug approved by USFDA for the treatment of acute schizophrenia in adults. Iloperidone shows poor oral bioavailability of about 36% as it undergoes extensive presystemic elimination. Benefits of nasal delivery, as an alternative approach, include non-invasiveness, accessibility, ease of administration and better compliance as compared to intravenous route. Delivery in small nasal volumes can be strengthened using drug nanosuspensions.

Objective

The objective of this study is to develop and evaluate Iloperidone nanosuspensions for nasal delivery to improve effectiveness in treating schizophrenia.

Methods

Iloperidone nanosuspensions containing Poloxamer 188 as stabilizer, Methocel K15M as mucoadhesive polymer and Gellan gum as gelling agent were prepared by wet milling. Process parameters such as the number of zirconium beads and rotations per minute were optimized to prepare nanosuspensions. The nanosuspensions were evaluated for particle size distribution, polydispersity, zeta potential, release, permeation and motor activity using animal models.

Results

The developed Iloperidone nanosuspensions showed average particle size and polydispersity index of 268.1 ± 2 nm and 0.362 ± 0.2, respectively and zeta potential of -19.2 ± 0.2 mV. release studies exhibited more than 80% drug release at the end of 6 hours, while studies indicated a greater percentage of drug from the nanosuspensions permeating across excised goat nasal mucosa. Studies in animal models depicted significant activity with improved motor response for Iloperidone nasal nanosupensions as compared to oral suspensions.

Conclusion

The present study demonstrated the successful development of Iloperidone nanosuspensions for nasal delivery in the management of schizophrenia and proposed to have commercial potential.

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Formulation Design and Evaluation of Iloperidone Nanosuspensions for Nasal Delivery using Wet-milling Approach
Curr Nanomed 15, 294 (2025); https://doi.org/10.2174/0124681873298851240702094437
/content/journals/cnanom/10.2174/0124681873298851240702094437
/content/journals/cnanom/10.2174/0124681873298851240702094437
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  • Article Type:     Research Article
Keyword(s): Iloperidone, in situ nasal, motor activity, goat nasal mucosa, schizophrenia, wet-milling

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