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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.
Annales Pharmaceutiques Francaises
|September 14, 2023
Summary
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.
