Development and Characterization of Transdermal Patch of Modified form of Brexpiperazol

Aim: Brexpiprazole (BPZ) is a typical antipsychotic drug used for the treatment of schizophrenia and depression. It is classified under BCS class-II with low aqueous solubility and high intestinal permeability. In the present investigation, a solid dispersion of BPZ was prepared to improve the solubility. A transdermal patch was optimized using the central composite design to control the delivery of BPZ.

Place and Duration of Study: The formulation was prepared and characterized at K. B. Institute of Pharmaceutical Education and Research, Gandhinagar, Gujarat, India during January 2021 to September 2021.

Methodology: A solid dispersion of BPZ was prepared using PEG 6000.A transdermal patch of BPZ was prepared and optimized using central composite design. Independent variables were fixed as ratio of RLPO: RSPO=2:1 (X1) and conc. of plasticizer (Triacetin) %W/W of polymer (X2). Dependent variables were fixed as folding endurance% (Y1) and cumulative % drug release at 24, 48, 72 and 96 hrs respectively (Y2-Y5) for the optimization of transdermal patch of SD of BPZ. Optimized formulation was characterized fully for its safety and efficacy using ex- vivo permeation study, skin irritation study and stability study.

Result: The tensile strength of optimized patch was 2.1±0.045 Kg/cm2. The thickness and hardness of patch was 0.0478±0.025 and 80.54±2.64gm/mm. The moisture content and moisture uptake values were 5.2%±0.36 and 6.21±0.24% respectively. Drug content was found to be 99.41±2.64%. The flux value obtained from BRX-SD-TP was 0.06 µg/cm2h. The flux was very proximal to the desired flux value. Prepared formulation was non-irritant and stable.

Conclusion: From the findings it can be concluded that BRX-SD-TP was successfully developed for treatment of Schizophrenia.