β-Cyclodextrin complexation as an effective drug delivery system for meropenem

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Microbiology

Background:

• Meropenem is a crucial antibiotic, but its stability in aqueous solutions and solid phases can be a challenge for drug delivery.
• Cyclodextrins, like beta-cyclodextrin, are known for their ability to form inclusion complexes with various molecules, potentially improving their properties.

Purpose of the Study:

• To prepare and characterize an inclusion complex of beta-cyclodextrin and meropenem.
• To evaluate the impact of complexation on meropenem's stability, release profile, and antimicrobial activity.
• To investigate the molecular interactions involved in the complex formation.

Main Methods:

• Preparation of the beta-cyclodextrin-meropenem inclusion complex.
• Characterization using Fourier-transform infrared spectroscopy (FT-IR), Raman spectroscopy, and differential scanning calorimetry (DSC).
• Stability studies in aqueous and solid phases.
• In vitro drug release studies over 20 hours.
• Microbial activity evaluation against clinically important bacterial strains.
• Molecular modeling for theoretical studies.

Main Results:

• The inclusion complex formation significantly enhanced the stability of meropenem in both aqueous and solid states.
• Sustained release of meropenem from the cyclodextrin cavity was observed, maintaining a constant concentration for 20 hours.
• The complexation did not impede meropenem's bactericidal action and even showed increased growth inhibition against certain strains.
• Molecular modeling suggested that the carbonyl groups of meropenem are involved in complex formation with beta-cyclodextrin.

Conclusions:

• The beta-cyclodextrin-meropenem inclusion complex is a promising drug delivery system, significantly improving meropenem's stability and prolonging its therapeutic effect.
• The enhanced antimicrobial activity observed highlights the potential clinical benefits of this complexed formulation.
• The findings support the role of meropenem's carbonyl groups in complexation, validated by both experimental and theoretical approaches.