Design Development and Optimization of Novel Long-Acting In-Situ Gel Formulation of Cariprazine Hydrochloride

Abstract

The aim of the present research work was to formulate and evaluate the novel long-acting In-Situ gel formulation of Cariprazine Hydrochloride (CPZ). Polaxamer Kolliphor P 407 and Polaxamer Kolliphor P 188 were used as thermo-sensitive extended-release polymers. Hydroxypropyl methyl Cellulose was used as a viscosity modifier/release retarding polymer, Carbopol was used gelling agent, and Tween 80 as a Surfactant. The In-Situ gel was formulated with the objectives of increasing contact time, achieving controlled release, reducing the frequency of administration and obtaining greater therapeutic efficacy of the drug. The prepared In-Situ gels were further optimized using physicochemical and chemical parameters like Solgel transition Time, Solgel transition temperature, Viscosity and In-Vitro drug release. Statistical optimization was performed using quality by design approach with Placket Burman DOE model and Design space was established for the optimized formulation. Stability study was conducted for optimized Cariprazine hydrochloride In-Situ gel formulation at optimum and controlled storage conditions. It was evident from these studies that the polymeric In-Situ gels formed were transparent and clear, and possessed a satisfactory gelling capacity.