Formulation, Evaluation, and Pharmacodynamic Investigation of Ziprasidone-b-cyclodextrin In-Situ Nasal Gel

Abstract

Ziprasidone hydrochloride is an atypical antipsychotic agent with an anti-schizophrenic activity having less solubility and less bioavailability. The nasal route acts as a promising delivery route for CNS targeting drugs due to improved bioavailability and can reduce peripheral side effects. The main aim of the study is to prepare an in-situ nasal gel of ziprasidone-β-cyclodextrin for improvement in the bioavailability of the drug. The in-situ gel was optimized using box-Behnken design. The optimized formulation was evaluated for homogeneity, viscosity, gelation temperature, mucoadhesive strength, in-vitro permeation studies. The pharmacodynamic activity of in-situ nasal gel was checked using the locomotor activity model. According to the statistical analysis of the design expert software, all the models were found significant. The pharmacodynamic investigation of the cyclodextrin mediated in situ nasal gel showed improvement in drug activity compared to a drug, drug-complex given by oral route indicating the nasal delivery of antipsychotic drug improves its effect.

Excipients Used for Modified Nasal Drug Delivery: A Mini-Review of the Recent Advances

“…Poloxamers (407 and 188) were selected as gelling agents; polyethylene oxide was also used to induce gelation and HPMC K4M to improve mucoadhesive strength. The results indicated significant release and mucoadhesion that confirmed adequate residence time at the site of action [ 40 ]. For a longer residence time in the nasal cavity, which could lead to increased bioavailability of geniposide, researchers formulated an in situ gel using poloxamers (P407, P188) and HPMC.…”