Different synthetic methodologies for achieving the most reliable synthetic pathway for the synthesis of pioglitazone-loaded poly(lactic-co-glycolic acid) (PLGA) polymeric nanoparticles were evaluated. The results of nanoprecipitation and single emulsion-evaporation methods were reported. The resulting systems regarding their size, Z-potential, entrapment efficiency, drug loading, storage times, drug release kinetics and costs were compared and characterized.
Recent findings have proved the benefits of Pioglitazone (PGZ) against atherosclerosis and type 2 diabetes.[1] Since the systematic and controllable release of this drug is of significant importance, encapsulation of this drug in nanoparticles (NPs) can minimize uncontrolled issues.[2] In this context, drug delivery approaches based on several poly(lactic-co-glycolic acid) (PLGA) nanoparticles have been rising in popularity due to their promising capabilities.[3] However, a fully reliable and reproducible synthetic methodology is still lacking. Todaro et al. presented a rational optimization of the most critical formulation parameters for the production of PGZ-loaded PLGA NPs by the single emulsification-solvent evaporation or nanoprecipitation methods.[4] The influence of several variables (e.g., component concentrations, phases ratio, injection flux rate) on the synthesis of the PGZ-NPs were examined. In addition, a comparison of these synthetic methodologies in terms of nanoparticle size, polydispersity index (PDI), zeta potential (ζp), drug loading (DL%), entrapment efficiency (EE%), and stability were offered. According to the higher entrapment efficiency content, enhanced storage time and suitable particle size, the nanoprecipitation approach appears to be the simplest, most rapid and most reliable synthetic pathway for these drug nanocarriers. More, a very slow drug release in PBS for the best formulation obtained by this synthesis were demonstrated. A possible future perspective is the development of an efficient targeted delivery system, both providing fluorophore-labelled NPs as imaging agent and aiming at delivering drugs to particular genes or proteins that are overexpressed or specific to malignant cells.[5][6] Moreover, these synthetic methods could be translated into a microfluidic system, since this allows a continuous production of NPs and reduces batch-to-batch variability, offering a more easily standardization of the parameters.
This entry is adapted from the peer-reviewed paper 10.3390/ijms23052522