Long Acting Polycaprolactone Based Parenteral Formulation of Aripiprazole Targeting Behavioural and Biochemical Deficit in Schizophrenia

• Published in: Journal of pharmaceutical sciences Vol. 110; no. 5; pp. 2185 - 2195
• Main Authors: Kaur, Lavjot, Sinha, V.R.
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.05.2021
• Subjects: Aripiprazole; Behavioural activity; Biochemical; Long acting parenteral; Polymeric microparticles; Schizophrenia; Schizophrenia; Biochemical; Aripiprazole; Long acting parenteral; Behavioural activity; Polymeric microparticles
• ISSN: 0022-3549; 1520-6017
• DOI: 10.1016/j.xphs.2020.12.028

Schizophrenia is a neurodevelopmental disorder which is expressed in the form of disturbed behaviour and abnormal mental functions. Patient's non-adherence to the medicine is the main cause of failure of drug therapy and increases incidence of relapses. Thus, for successful management of disease long acting parenteral formulations were developed. Aripiprazole was encapsulated in biocompatible polycaprolactone microsphere by o/w emulsion solvent-evaporation method in order to achieve sustained release of the drug for several weeks after single subcutaneous administration. They were optimised on the basis of various parameters such as physical appearance, particle size (49.4 μm–387.1 μm), encapsulation efficiency (70%–95%), percentage yield (33%–75%) and drug loading (25.9%–47.5%). The surface topography and sphericity of the microspheres was determined by scanning electron microscopy which revealed that the microspheres formed were spherical and non-porous in nature. The in vitro releases from the selected formulations were found to be 87% and 95% respectively after 45 days of dissolution. In vivo efficacy of optimised formulation showed significantly (p < 0.05) amelioration of various positive, negative and cognitive symptoms associated with schizophrenia and oxidative stress markers in ketamine-induced schizophrenia model in rats for 30 days.