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Lidocaine and soyasterole-PEG-16-ether — investigations on the interaction between an amphiphilic drug and a nonionic surfactant in aqueous solution
Authors:St. Baade  C. C. Mueller-Goymann
Affiliation:(1) Institute of Pharmaceutical Technology and Biopharmacy, Philipps-University of Marburg, Germany;(2) Institute of Pharmaceutical Technology, University of Braunschweig, Germany;(3) Institut für Pharmazeutische Technologie, Technische Universität Carolo-Wilhelmina zu Braunschweig, Mendelssohnstr. 1, 38106 Braunschweig, Germany
Abstract:In order to study the interactions between the surface active local anaesthetic drug lidocaine and the nonionic surfactant soyasterole-PEG-16-ether firstly the self association of the drug in aqueous solution was investigated by different methods. Transmission electron microscopy hinted at micellization and surface tension measurements resulted in a CMC of 12.9% (salt form) and 0.08% (base form), respectively, whereas solubilization experiments, NMR spectroscopy and osmotic pressure measurements obviously disproved the existence of drug micelles. The detected CMC only meant a surface saturation and the TEM pictures probably showed artifacts. In diluted systems containing both drug and surfactant no formation of mixed micelles took place, as pointed out by the tensiometric determination of the CMC of the mixtures showing no minimum in the CMC/% drug-curve. Also, gel permeation chromatography clearly separated surfactant micelles and drug molecules. In contrast to this, evident interactions between the base form of the drug and the surfactant occurred when the drug concentration was increased: the dynamic viscosity of the systems rose distinctly, probably caused by growth of the surfactant associates to a more rodlike form. The salt form had nearly no influence on the viscosity of the preparations.
Keywords:Nonionic surfactants  lidocaine  micelles  interactions  surface tension  viscosimetry  gel permeation chromatography (PGC)
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