Formulation of Amisulpride loaded Nanoemulsion Drug Delivery System for the Treatment of Schizophrenia

Abstract

The treatment of schizophrenia has advanced because the therapeutic efficacy, tolerability, and safety profiles of atypical antipsychotics. Amisulpride is an atypical antipsychotic drug, effective for positive and negative symptoms of schizophrenia with unique receptor pharmacology. As could be predicted from the pharmacologic profile of a pure D2/D3 receptor blocker. Nanoemulsion formulation containing Amisulpride was developed by ultra sonication method. Formulations were prepared using oil (oleic acid and IPM), two surfactants ( Labrasol, and Tween 20 “Smix”) and co-surfactant (PEG 400). Optimized formulation, containing 10% oil, 2:1 as Smix, co-surfactant ratio 1 and 2 as ratio of Labrasol and Tween-20 in Smix was prepared. Amisulpride is practically insoluble in water and suffers from irregular and low bioavailability (48%). The current study is aimed at developing and optimizing a Nanoemulsion formulation of amisulpride in order to improve oral absorption of amisulpride through GIT. It exhibited faster and more complete dissolution of amisulpride than marketed tablet regardless of the type and pH of the dissolution medium. Also, it showed a significant improvement of the bioavailability of amisulpride in rats. Optimized Nanoemulsion showed significant (p<0.001) increase in vivo bioavailability. Keywords: Amisulpride, Nanoemulsion formulation, phase diagram, pharmacokinetic, Schizophrenia.