Abstract:
:Some lipophilic fluoro-substituted N-benzoyl-2-aminobenzothiazole antibacterial agents have been evaluated for their activity in the presence of cyclodextrins (CDs) containing aqueous solutions where CDs are adopted as solubilizing excipients for improving the poor water solubility of these compounds. For such purpose both the natural β-CD and one of FDA/EMA approved CDs for parenteral use (i.e. HP-β-CD) have been employed. The solubility rank order observed was accounted for by thermal analysis (Differential Scanning Calorimetry) and FT-IR spectroscopy. The most promising compound was subjected to further NMR spectroscopic studies and molecular modelling simulations to verify the interactions between the guest molecule and the CD cavity. The assessment of the antibacterial activity of such compounds against selected Gram positive and Gram negative bacterial strains clearly showed that their antimicrobial effectiveness may, quite in all instances, be positively affected by complexation with β-CD and HP-β-CD. These results, which are in some ways in contrast with those already reported in the literature, are herein discussed on the basis of plausible mechanisms. Moreover, this investigation also reveals that the described methodology of complexing both lipophilic and hydrophilic antimicrobial agents with CDs may be an useful approach to enhance their effectiveness as well as a promising strategy to overcome even the microbial resistance problem.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Trapani A,De Laurentis N,Armenise D,Carrieri A,Defrenza I,Rosato A,Mandracchia D,Tripodo G,Salomone A,Capriati V,Franchini C,Corbo Fdoi
10.1016/j.ijpharm.2015.11.024subject
Has Abstractpub_date
2016-01-30 00:00:00pages
18-22issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(15)30370-7journal_volume
497pub_type
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