Review on cyclodextrin multicomponent complexes

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Based on 109 references this paper gives an overview on how the addition of an auxiliary substance forming multicomponent complexes can enhance complexation efficiency and facilitate the therapeutic applicability of different drugs (1). This review discusses multicomponent complexation using amino acids; organic acids and bases; and water-soluble polymers as auxiliary excipients. Special attention is given to improved properties by including information on the solubility, dissolution, permeation, stability and bioavailability of several relevant drugs. In addition, the use of multicomponent CD complexes to enhance therapeutic drug effects is summarized.

y. The multicomponent complexes of CD with organic acids or bases, amino acids and polymers have proven to be very useful for improving and controlling properties of ionizable, weakly ionizable and non-ionizable drugs. In general, the most suitable auxiliary agent and the most appropriate CD should be selected by considering the particular drug’s physicochemical properties and the characteristics to optimize. For example, in the case of acidic drugs, the basic auxiliary agent TEA has been demonstrated to significantly enhance both the solubility and the permeability. Regarding using amino acids as auxiliary agents, arginine is the most used compound, since in general it shows a synergistic effect with the CD toward enhancing drug solubility.

Mayank Patel, Rajashree Hirlekar (2019) Multicomponent cyclodextrin system for improvement of solubility and dissolution rate of poorly water soluble drug, Asian Journal of Pharmaceutical Sciences, 14, 104-115,

(1) Aiassa, V.; Garnero, C.; Longhi, M.R.; Zoppi, A. Cyclodextrin Multicomponent Complexes: Pharmaceutical Applications. Pharmaceutics 2021, 13, 1099.

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