Journal
BIOMOLECULES
Volume 10, Issue 1, Pages -Publisher
MDPI
DOI: 10.3390/biom10010024
Keywords
cefuroxime axetil; cyclodextrin; molecular modeling
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Funding
- program Diamond Grant
- PL-Grid Infrastructure
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This study aimed to investigate changes in the solubility and antimicrobial efficacy of cefuroxime axetil (CA) when incorporated into cyclodextrin (CD). While choosing the CD, the validated in silico model was used. A theoretical model based on docking and molecular mechanics/generalized born surface area was validated using a curated dataset of API (active pharmaceutical ingredient)-CD stability constants. The library of commonly used cyclodextrins was virtually screened, indicating CA -hydroxypropyl-beta CD (HP beta CD) as the most thermodynamically favored system. Solid-state CA-HP beta CD system was prepared and characterized by differential scanning calorimetry (DSC), Fourier-transform infrared (FT-IR), and X-ray diffraction (XRPD) methods. The dissolution profiles of the CA and its cyclodextrin system were evaluated. Microbiological activity of the CA-HP beta CD inclusion system was studied based on changes in minimal inhibitory concentration (MIC) values and related to ones of the pure CA. The theoretical model was successfully validated, obtaining an average correlation with experimental data R = 0.7. The dissolution study showed significantly improved dissolution profiles of CA-HP beta CD compared to CA. HP beta CD increases the antimicrobial efficacy of CA up to 4-fold compared to pure CA.
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