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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 in situ 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, in vitro release, ex-vivo 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. in vitro release studies exhibited more than 80% drug release at the end of 6 hours, while ex-vivo 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.
Palshetkar et al. (Mon,) studied this question.