Preparation, Characterization, and Properties of Inclusion Complexes of Balofloxacin with Cyclodextrins
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The study mainly aimed to improve the aqueous solubility of Balofloxacin (BLFX) by preparing the inclusion complexes (ICs) of BLFX with cyclodextrins (CDs). In this study, ICs in solid state were obtained by using beta-CD (β-CD), 2-hydroxypropyl-β-CD (HP-β-CD), 2, 6-dimethyl-β-CD (DM-β-CD) through a freeze-drying technique. The formation of ICs was confirmed through Fourier-transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffraction, nuclear magnetic resonance, and scanning electron microscopy. Results demonstrated that the water solubility and dissolution rates of three ICs were distinctly improved than that of parent BLFX. Bacteriostatic experiment manifested that the antibacterial effect of BLFX was not inhibited after encapsulation in CDs. The damage of BLFX to kidney and liver cells was reduced. Consequently, successful preparation of the ICs of BLFX with CDs provided possibility for devising new dosage form of BLFX, which held great promise for further applications in clinical fields.
KEY WORDSbalofloxacin cyclodextrin inclusion complex solubility cytotoxicity
We appreciated Hui Wang and Yueming Zhai from the Analytical & Testing Center of Sichuan University for helping with SEM and NMR characterization, respectively.
This work was supported by Sichuan Science and Technology Program (Grant No. 2018JY0188) and the Fundamental Research Funds for the Central Universities (Grant No. 2018SCU12043).
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