Vancomycin-triacetyl cyclodextrin interaction products for prolonged drug delivery.

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Materials Science

Background:

• Site-specific delivery of antibiotics like vancomycin (VCM) is crucial for treating bone infections.
• Hydrophobic cyclodextrins (TACD) offer potential for modifying drug release profiles.
• Understanding the influence of preparation techniques on VCM-TACD interactions is key for developing effective drug delivery systems.

Purpose of the Study:

• To investigate the interaction between vancomycin (VCM) and three hydrophobic triacetyl cyclodextrins (TACD).
• To evaluate the role of preparation techniques (kneading, coevaporation, spray drying) in forming VCM-TACD interaction products.
• To assess the potential of these products for prolonged drug delivery in site-specific bone infection treatments.

Main Methods:

• Preparation of physical mixtures and binary systems of VCM with triacetyl alpha-, beta-, or gamma-cyclodextrin (TAαCD, TAβCD, TAγCD) using kneading, coevaporation, and spray drying.
• Characterization of systems using thermal analysis (TG, DSC), HPLC for drug content, and Franz cell for in vitro drug release.
• Evaluation of particle size and drug-loading efficiency for parenteral administration suitability.

Main Results:

• All preparation methods yielded VCM-TACD systems with suitable particle size and near 100% drug loading, indicating VCM stability.
• The kneading method with TAαCD and coevaporation with TAβCD showed prolonged VCM release.
• Spray drying from aqueous suspensions failed to form interaction products; however, spray drying from hydroacetonic solutions consistently reduced VCM release, particularly with TAγCD, due to VCM-TACD interactions.

Conclusions:

• Preparation technique significantly impacts VCM release from TACD systems.
• Spray drying from hydroacetonic solutions is effective in forming VCM-TACD interaction products that prolong drug release.
• The VCM-TAγCD interaction product obtained via spray drying from hydroacetonic solutions shows significant promise for developing parenteral site-specific delivery systems for vancomycin, maintaining its antimicrobial activity.