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PLGA-based microspheres loaded with metformin hydrochloride: Modified double emulsion method preparation,
Priyanka Chauhan1, Himanshu Paliwal2, Chetan Singh Chauhan1
1Faculty of Pharmacy, Bhupal Nobles' University, Udaipur, Rajasthan, India.
Abstract:
The modified solvent removal method was used to encapsulate metformin hydrochloride (MH) within poly(lactic-co-glycolic acid) (PLGA) microspheres. The study investigated 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 4.4μm to 2.7μm. 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 differences 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.
Insights
This study developed poly(lactic-co-glycolic acid) (PLGA) microspheres for metformin hydrochloride (MH) encapsulation. The amorphous state of encapsulated MH resulted in a slow, prolonged drug release over 24 days.
Area of Science:
- Materials Science
- Pharmaceutical Sciences
- Polymer Chemistry
Background:
- Poly(lactic-co-glycolic acid) (PLGA) is a biodegradable polymer widely used in drug delivery systems.
- Metformin hydrochloride (MH) is a first-line medication for type 2 diabetes, often requiring controlled release formulations.
- Developing effective encapsulation methods for sustained drug delivery is crucial for improving therapeutic outcomes.
Purpose of the Study:
- To encapsulate metformin hydrochloride (MH) into poly(lactic-co-glycolic acid) (PLGA) microspheres using a modified solvent removal method.
- To investigate the impact of varying PLGA concentrations on drug loading and release kinetics.
- To characterize the physical state of MH within the microspheres and correlate it with drug release profiles.
Main Methods:
- Double emulsion solvent removal technique for microsphere preparation.
- Particle size analysis to determine microsphere dimensions.
- Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), and X-ray Diffraction (XRD) for material characterization.
- In vitro drug release studies over a 24-day period.
Main Results:
- Microsphere particle diameters ranged from 2.7μm to 4.4μm.
- High encapsulation efficiencies (81-90%) and drug loadings (11-18%) were achieved.
- Drug release exhibited a biphasic pattern over 24 days, with near-complete release by study's end.
- FTIR showed no significant MH-PLGA interactions; DSC and XRD indicated MH was molecularly dispersed and amorphous within the microspheres.
Conclusions:
- The modified solvent removal method effectively produced MH-loaded PLGA microspheres with high encapsulation efficiency.
- The amorphous state of encapsulated MH is likely responsible for the observed slow and prolonged drug release.
- These findings support the potential of PLGA microspheres for controlled delivery of metformin hydrochloride.
