Revolutionizing Aripiprazole Delivery: Improving Solubility and Permeation Via Solid dispersion and In-situ Intranasal Gelling Systems

Document Type

Article

Publication Date

4-2025

Abstract

Aripiprazole (ARI) is a class IV drug of poor solubility and permeability. This study focused on improving the ARI solubility and permeability via solid dispersion technique (SDs), which was further loaded through intranasal in-situ gel to target the brain directly. ARI- SDs were prepared by Solvent evaporation technique. SD9 was the optimum solid dispersion that enhanced the solubility of ARI by 6.5 folds and selected for preparation of in-situ intranasal gel using Chitosan and HPMC K15M. A 33 factorial design was utilized to optimize the percentage of drug released after 24 h, gelation time and gelation temperature. The gel formulations were investigated for pH, viscosity, drug content%, gelation time and temperature, gel strength, gel spreadability, mucoadhesive strength and percentage of drug released after 24 h. The optimized formula has achieved 93.4 ± 0.74 % release of ARI after 24 h, a gelation time of 76 s and gelation temperature of 33.2OC. The optimized formula was then investigated for ex-vivo permeation, nasal ciliotoxicity and showed a 7.5 folds permeability enhancement compared to ARI suspension without any sign of intranasal mucosal damage. In conclusion, the prepared in-situ gel of ARI would be a good alternative to oral delivery for schizophrenic patients.

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