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Drug loading in cyclodextrin polymers: dexamethasone model drug

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Abstract

In pharmaceutical formulations cyclodextrins (CDs) are used to improve the aqueous solubility, stability, dissolution rate, bioavailability and/or local tolerance of drugs. Moreover, water-soluble polymers can be used to stabilize drug/CD complexes through formation ternary complexes. Alternative approach is to use CD-polymers, which can both enhance the aqueous solubility of a drug and result in sustained drug release. The aim of this work was to compare the solubilizing effects of ternary drug/CD/polymer complexes with two novel high molecular weight CD-polymers, i.e. poly(ethylene glycol) based γ-cyclodextrin (γCD) polymer (PEG/γCD) and epichlorohydrin-γ-cyclodextrin polymer (EPI/γCD) using dexamethasone (Dex) as a model drug, as well as the drug loading capacity of those selected CD-polymers. Hydroxypropyl methylcellulose and carboxymethylcellulose sodium salt were shown to have negligible effect on the solubilizing efficacy of γCD while hexadimethrine bromide increases the solubilization efficacy. The stability of the polymers was tested and it was adequate for the experimental conditions used. The solubilization efficacy of both CD-polymers was higher than that of the parent γCD and these γCD based polymers are able to load greater amount of Dex than the parent γCD.

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Acknowledgements

This work was supported by The Icelandic Centre for Research (RANNÍS).

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Authors and Affiliations

  1. Faculty of Pharmaceutical Sciences, University of Iceland, Hofsvallagata 53, 107, Reykjavik, Iceland

    Maria D. Moya-Ortega, Martin Messner, Phatsawee Jansook, Hákon H. Sigurdsson & Thorsteinn Loftsson

  2. Section of Chemistry, Department of Biotechnology, Chemistry and Environmental Engineering, Aalborg University, Sohngaardsholmsvej 57, 9000, Aalborg, Denmark

    Thorbjørn Terndrup Nielsen & Kim Lambertsen Larsen

  3. Laboratoire de Recherche sur les Polymères, LRP, CNRS, UMR 7581, 2-8 Rue Henri Dunant, 94320, Thiais, France

    Veronique Wintgens & Catherine Amiel

Authors
  1. Maria D. Moya-Ortega
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  2. Martin Messner
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  3. Phatsawee Jansook
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  4. Thorbjørn Terndrup Nielsen
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  5. Veronique Wintgens
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  6. Kim Lambertsen Larsen
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  7. Catherine Amiel
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  8. Hákon H. Sigurdsson
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  9. Thorsteinn Loftsson
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Correspondence to Thorsteinn Loftsson.

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Moya-Ortega, M.D., Messner, M., Jansook, P. et al. Drug loading in cyclodextrin polymers: dexamethasone model drug. J Incl Phenom Macrocycl Chem 69, 377–382 (2011). https://doi.org/10.1007/s10847-010-9758-8

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  • DOI: https://doi.org/10.1007/s10847-010-9758-8

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