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Open AccessArticle

Computer-Aided Design of Cefuroxime Axetil/Cyclodextrin System with Enhanced Solubility and Antimicrobial Activity

Department of Pharmacognosy, Faculty of Pharmacy, Poznań University of Medical Sciences, Święcickiego 4, 60-781 Poznań, Poland
Department of Biotechnology and Food Microbiology, Poznan University of Life Sciences, Wojska Polskiego 48, 60-627 Poznan, Poland
Institute of Molecular Physics, Polish Academy of Science, ul. Smoluchowskiego 17, 60-179 Poznań, Poland
Poznan University of Technology, Institute of Materials Science and Engineering, Pl. M.Sklodowskiej-Curie 5, 60-965 Poznan, Poland
Department of Pharmacology, Medical University of Lublin, Chodźki 4a, 20-093 Lublin, Poland
Department of Chemical Technology of Drugs, Poznan University of Medical Sciences, Grunwaldzka 6, 60-780 Poznan, Poland
Author to whom correspondence should be addressed.
Biomolecules 2020, 10(1), 24;
Received: 11 December 2019 / Revised: 20 December 2019 / Accepted: 20 December 2019 / Published: 23 December 2019
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-βCD (HPβCD) as the most thermodynamically favored system. Solid-state CA–HPβCD 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–HPβCD 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–HPβCD compared to CA. HPβCD increases the antimicrobial efficacy of CA up to 4-fold compared to pure CA. View Full-Text
Keywords: cefuroxime axetil; cyclodextrin; molecular modeling cefuroxime axetil; cyclodextrin; molecular modeling
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Mizera, M.; Szymanowska, D.; Stasiłowicz, A.; Siąkowska, D.; Lewandowska, K.; Miklaszewski, A.; Plech, T.; Tykarska, E.; Cielecka-Piontek, J. Computer-Aided Design of Cefuroxime Axetil/Cyclodextrin System with Enhanced Solubility and Antimicrobial Activity. Biomolecules 2020, 10, 24.

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