Michał Krzysztof Kołodziejczyk, Michał Jakub Nachajski, Marek Lukosek, Marian Mikołaj Zgoda

Surface activity of novel surface active compounds, products of catalytic oxyethylation of cholic acid and their micellar adducts with selected lipophilic therapeutic agents
2014-02-17

Abstract: The aim of this study was to determine the surface activity parameters of novel surface active compounds, products of catalytic oxyethylation of cholic acid, and their micellar adducts with selected lipophilic therapeutic agents (diclofenac, loratadine, naproxen and rutin). High solubility of lipophilic naproxen was observed in the environment of aqueous solutions of the cholic acid oxyethylation products as suggested by determined factual solubility and the value of micellar partition coefficient (Kw m). Determined surface activity of surfactants described by various physicochemical characteristics (γcmc 25 , cmc, ΔGm o and Am) suggested their compatibility with physiological values of the surface activity of plasma (48.0-52.0 mJ/m2) and lacrimal fluid (46.0-52.0 mJ/m2). Calculated values of HLB1 HNMR and nTE of the micellar adduct in solid phase (solid dispersion) corresponded to an increase in its hydrophilicity, and, therefore, suggested possible mechanisms and site of diclofenac, loratadine, naproxen and rutin solubilization in the micellar structure (core or palisadic layer).

Keywords: solubilization, surface activity, diclofenac, loratadine, naproxen, rutin, ethoxylation products of cholic acid