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  • Title: Effect of 4-sulphonato-calix[n]arenes and cyclodextrins on the solubilization of niclosamide, a poorly water soluble anthelmintic.
    Author: Yang W, de Villiers MM.
    Journal: AAPS J; 2005 Sep 02; 7(1):E241-8. PubMed ID: 16146345.
    Abstract:
    The present study investigated the effect of water-soluble 4-sulphonato-calix[n]arenes, cyclodextrins, and combinations of these macromolecules on the aqueous solubility of a poorly water-soluble drug, niclosamide. Complexation between the macromolecules and niclosamide was confirmed by thermal analysis and phase solubility studies in a pH 7.0 Mcllvaine buffer kept at 30 degrees C. Results show that the increase in solubility ranked as follows: 4-sulphonato-calix[6]arene + hydroxypropyl-beta-cyclodextrin (HP-beta-CD) > 4-sulphonato-calix[6]arene + beta-cyclodextrin > 4-sulphonato-calix[6]arene + gamma-cyclodextrin = HP-beta-CD > 4-sulphonato-calix[6]arene > 4-sulphonato-calix[8]arene = 4-sulphonato-calix[4]arene > beta-cyclodextrin . Type B phase solubility profiles were observed, indicating a decrease in solubility at concentrations > 0.004 to 0.005 mol/L of the 4-sulphonato-calix[n]arenes or combinations of 4-sulphonato-calix[6]arene and the cyclodextrins. However, below this concentration, the greatest increase in the aqueous solubility niclosamide was observed when 4-sulphonato-calix[6]arene and HP-beta-CD were combined. This increase in solubility was additive.
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