Abstract

Sustained drug release formulation in in-vivo for prolonged time is very helpful in keeping medical adherence and patient compliance in psychotic illness such as schizophrenia and bi-polar depression. Based on this clinical need, we developed PLGA microparticles (MS) by supercritical anti-solvent process that efficiently encapsulate Aripiprazole (an atypical antipsychotic drug; well known for having a lower risk of hyperprolactinemia and a low potential for metabolic disturbances). The developed MS having spherical shape with smooth surface (confirmed by SEM) and showing zero order drug release for 5 weeks. For formulation optimization and understanding of release study, the MS were investigated for drug distribution in the PLGA matrix, drug release and degradation kinetics in vitro as a step-up for later in vivo application. The drug distribution was studied by XRD and DSC analysis that further validated by near infrared (NIR) imaging. MS degradation profiles (an important indicative of drug influence on PLGA degradation rate) during the release period were estimated by measuring the change in glass transition temperature (Tg in °C) and polymer molecular weight (Mw) using DSC and gel permeation chromatography (GPC) respectively.