Preparation and Characterization of Intramuscular PLGA Based Microsphere

Abstract

The current studies was design and evaluate biodegradable PLGA microspheres for sustained or extended release, with primary goal of avoiding combination of oral therapy for the treatment of schizophrenia. PLGA copolymers 75:25 was used to prepare four microsphere formulations of anti-psychotic drug Olanzapine. The microspheres were characterized by in-vitro dissolution and other physio-chemical methods. A simulation of multiple dosing at weekly or 15-day regimen revealed pulsatile behavior for all formulations with steady state may be achieved by the second dose. Overall, the in-vitro study of Formulations 001, 002, 003, or 004 will eliminate the need for combination oral therapy and reduce time to achieve steady state, with a smaller washout period upon duration of therapy. Results of this study prove the suitability of using PLGA 75:25 copolymers of different composition and molecular weight to produce sustained or extended release formulations that can enhance pharmacological effectiveness for anti-psychotic intra-muscular administration of Olanzapine.

Keywords: sustained release, PLGA microspheres, Olanzapine