Abstract
Inclusion complexes using α-, β-, γ-, and hydroxypropyl-β-CD (HP-β-CD) were produced with the antibiotic enrofloxacin, with the aim of increasing its solubility by complexation. Phase solubility diagrams were obtained, to confirm the formation of inclusion complexes, and to determine the solubility enhancement and stability constant of each complex. Enrofloxacin inclusion in β-CD showed the highest value of the complex stability constant (35.56 mmol L−1), but the greatest increase in solubility was obtained using HP-β-CD reaching a 1258% increase over enrofloxacin solubility in the absence of CD. The order of highest enrofloxacin solubility achieved was: HP-β-CD > α-CD > γ-CD > β-CD. In addition, formation of complexes was confirmed by differential scanning calorimetry and thermogravimetry, applied to the complexes obtained by the kneading technique. The influence of citric acid, alone or as an adjunct of β-CD, on the solubility of enrofloxacin was also determined. A solution of 15 mmol L−1 citric acid dissolved 10 g L−1 of enrofloxacin, but a gradual increase in β-CD concentration in the presence of citric acid did not increase the degree of solubilization of enrofloxacin.
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The authors thank CNPq (Conselho Nacional de Desenvolvimento Científico e Tecnológico), CAPES (Coordenação de Aperfeiçoamento de Pessoal de Nível Superior), and Fundação Araucária for financial support, and Formil Química Ltda for the gift of enrofloxacin.
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Calsavara, L.P.V., Zanin, G.M. & de Moraes, F.F. Enrofloxacin inclusion complexes with cyclodextrins. J Incl Phenom Macrocycl Chem 73, 219–224 (2012). https://doi.org/10.1007/s10847-011-0045-0
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DOI: https://doi.org/10.1007/s10847-011-0045-0