Solubilizing Steroidal Drugs by Beta-Cyclodextrin Derivatives

    Dennis H. Schwarz, Annegret Engelke, Gerhard Wenz
    TLDR Using β-cyclodextrin derivatives improves the solubility and bioavailability of steroidal drugs.
    The study investigated the solubilization of 7 steroidal drugs using 6 different β-cyclodextrin (β-CD) derivatives. The anionic β-CD thioether HSES provided the highest concentrations of dissolved steroids (around 19 mM for 4 wt.% of HSES) but exhibited low specificity. In contrast, the neutral β-CD thioethers HTMT and HTG showed specific binding to testosterone and β-estradiol, respectively. HSES was identified as a promising candidate for new formulations of estradiol, finasteride, prednisone, and dexamethasone, potentially improving their solubility and bioavailability.
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