A review of recent applications of cyclodextrins for drug discovery

ISSN： 1354-3776

Source： Expert Opinion on Therapeutic Patents, Vol.9, Iss.12, 1999-12, pp. : 1697-1717

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Abstract

This review summarises the pharmaceutical applications of cyclodextrins (CDs), particularly including the patent literature 1996 - 1999. To place these developments in context there is an introduction to the previously reported molecular and supramolecular (complex formation) properties of CDs and their biological properties, and clinical applications, which mainly involve drug (re)formulation. The growing utility of CDs as pharmaceutical excipients is discussed in three main categories. Firstly, complexes formed between CDs and previously known drugs wherein the new conjugate confers improved efficacy or reduced side effects. Secondly, conjugates conferring improved aqueous solubility and thirdly, a miscellaneous category including conjugates with new compounds. In addition, the emerging areas of covalently bound CD-drug complexes and potential applications of CDs acting directly as medicinal agents in their own right are reviewed. In some of these applications chemically modified CDs are found to augment the patentability and properties of the well known -, &bgr;- and &ggr;-CDs. The chemical structures of these novel CDs are discussed together with the challenge of their synthesis and purification. During the period covered by this review the number of patents and publications describing therapeutic applications of CDs has continued to grow whilst the industrial production of this fascinating class of supramolecular compounds has increased substantially leading to a corresponding fall in price.