International Journal of Molecular Sciences | |
β-Cyclodextrin Inclusion Complex to Improve Physicochemical Properties of Pipemidic Acid: Characterization and Bioactivity Evaluation | |
Rosa Iacovino1  Filomena Rapuano2  Jolanda Valentina Caso1  Agostino Russo1  Margherita Lavorgna1  Chiara Russo1  Marina Isidori1  Luigi Russo1  Gaetano Malgieri1  | |
[1] Department of Environmental, Biological and Pharmaceutical Sciences and Technologies, Second University of Naples, Via A. Vivaldi 43, 81100 Caserta, Italy; E-Mails:;Department of Biological and Environmental Science, University of Sannio, Via Port’Arsa 11, 82100 Benevento, Italy; E-Mail: | |
关键词: β-cyclodextrin; pipemidic acid; inclusion complex; microbial activity; antitumoral activity; | |
DOI : 10.3390/ijms140713022 | |
来源: mdpi | |
【 摘 要 】
The aptitude of cyclodextrins (CDs) to form host-guest complexes has prompted an increase in the development of new drug formulations. In this study, the inclusion complexes of pipemidic acid (HPPA), a therapeutic agent for urinary tract infections, with native β-CD were prepared in solid state by kneading method and confirmed by FT-IR and 1H NMR. The inclusion complex formation was also characterized in aqueous solution at different pH via UV-Vis titration and phase solubility studies obtaining the stability constant. The 1:1 stoichiometry was established by a Job plot and the inclusion mechanism was clarified using docking experiments. Finally, the antibacterial activity of HPPA and its inclusion complex was tested on
【 授权许可】
CC BY
© 2013 by the authors; licensee MDPI, Basel, Switzerland
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