Formulation composition, manufacturing process, and characterization of poly(lactide-co-glycolide) microparticles

Injectable long-acting formulations, specifically poly(lactide-co-glycolide) (PLGA) based systems, have been used to deliver drugs systemically for up to 6 months. Despite the benefits of using this type of long-acting formulations, the development of clinical products and the generic versions of existing formulations has been slow. Only about two dozen formulations have been approved by the U.S. Food and Drug Administration during the last 30 years. Furthermore, less than a dozen small molecules have been incorporated and approved for clinical use in PLGA-based formulations. The limited number of clinically used products is mainly due to the incomplete understanding of PLGA polymers and the various variables involved in the composition and manufacturing process. Numerous process parameters affect the formulation properties, and their intricate interactions have been difficult to decipher. Thus, it is necessary to identify all the factors affecting the final formulation properties and determine the main contributors to enable control of each factor independently.