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Inclusion complexes of 5-flucytosine with β-cyclodextrin and hydroxypropyl-β-cyclodextrin: characterization in aqueous solution and in solid state

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Abstract

Complexation between 5-flucytosine (5-FC), a cytosine analogue with in vitro antifungal and antiyeast activity, and β-cyclodextrins (β-cyclodextrin and hydroxypropyl-β-cyclodextrin) was studied in solution and in solid states. Complexation in solution was evaluated using solubility studies, UV–vis and 1H-NMR. In the solid state, differential scanning calorimetry (DSC), scanning electron microscopy (SEM), FT-IR and X-ray diffraction studies were used. UV–vis, FT-IR and 1H-NMR spectroscopy studies showed that the complex formed occurs by complexation of piridinique base analogue into inner cavity. DSC studies showed the existence of a complex of 5-FC with β-CDs. X-ray studies confirmed the DSC results of the complex existence. Solubility studies showed that the complexed drug is forty times more soluble than free 5-FC, indicating the obtained systems as future, promising drug carriers.

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Acknowledgment

This research was financial supported by Grant 2 CEex D11-106/2006 (CICLOMED).

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Authors and Affiliations

  1. Inorganic Polymers, Institute of Macromolecular Chemistry Petru Poni, Str. Gr Ghica Voda, no 41 A, Iasi, 711321, Romania

    Mariana Spulber, Mariana Pinteala, Adrian Fifere, Valeria Harabagiu & Bogdan C. Simionescu

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  1. Mariana Spulber
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  2. Mariana Pinteala
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  3. Adrian Fifere
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  4. Valeria Harabagiu
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  5. Bogdan C. Simionescu
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Correspondence to Mariana Spulber.

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Spulber, M., Pinteala, M., Fifere, A. et al. Inclusion complexes of 5-flucytosine with β-cyclodextrin and hydroxypropyl-β-cyclodextrin: characterization in aqueous solution and in solid state. J Incl Phenom Macrocycl Chem 62, 117–125 (2008). https://doi.org/10.1007/s10847-008-9446-0

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  • DOI: https://doi.org/10.1007/s10847-008-9446-0

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