Development and evaluation of sustained release injectable formulations of milnacipran and aripiprazole

Abstract

Parenteral formulation of aripiprazole and milnacipran was formulated for sustained delivery of drug. Aripiprazole loaded microparticles of PCL was formulated by o/w double emulsion technique with high entrapment efficiency and drug loading. The formulation was non-irritant and was found to be stable at room temperature and refrigerated temperature. Single dose of prepared microspheres delivers drug for 45 days with increased mean residence time and half-life. The behavioral studies showed improvement in positive, negative and cognitive symptoms of schizophrenia. Microsphere of milnacipran hydrochloride was formed with very low entrapment efficiency hence ISGFS of the drug was formulated with higher drug loading. Single subcutaneous injection of prepared ISGFS in rats has shown sustained released of drug over a period of 21 days with improved depression like symptoms such as anhedonia, anxiety, locomotor activity and helplessness as well as decrease in corticosterone level. It also significantly increases half-life and mean residence times of milnacipran hydrochloride as compared with the drug solution. Both drug formulations showed the efficacy for extended period after single injection. newline