PLGA-based microspheres loaded with metformin hydrochloride: Modified double emulsion method preparation, optimization, characterization, and in vitro evaluation

The modified solvent removal method was used to encapsulate metformin hydrochloride (MH) within poly(lactic-co-glycolic acid) (PLGA) microspheres. The study inves-tigated the effect of varying polymer concentrations on the loading and release of the drug from the microspheres. The encapsulation process involved using a double emulsion method, resulting in microspheres with particle diameters ranging from approximately 4.4 mu m to 2.7 mu m. The study achieved high encapsulation efficiencies, ranging from 81% to 90%, with drug loadings ranging from 18% to 11%. The release of the drug from the microspheres followed a biphasic pattern over 24 days, with nearly complete release by the end of the study period. Fourier transform infrared spectroscopy (FTIR) analysis indicated that there were no notable differ-ences between PLGA and MH-loaded microspheres, suggesting minimal interactions between MH and PLGA. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) techniques were used to investigate the state of the MH within the microspheres. The results suggested that the MH was dispersed at a molecular level within the spheres and existed in an amorphous state. This amorphous state of the drug may explain the slow and prolonged release observed in the study. (c) 2023 Published by Elsevier Masson SAS on behalf of Academie Nationale de Pharmacie.