INVESTIGATIONS ABOUT HEMOLYSIS AND SOLUBI LIZATION BEHAVIOR OF NONIONIC POLYMERIC SURFACTANTS

The solubilization of poorly water soluble drugs in surfactant solutio ns is still a problem in pharmaceutical technology. There doesn't exis t any surfactant which can be applied unrestricted in parenteral dosag e forms. For this reason, alkylpolyglycosides and fatty esters of dext ran were investigated. Their solubilization behaviour and hemolytic ac tivity was tested and compared to established surfactants. For solubil ization, only water soluble surfactants can be used. That means, that only alkylpolyglycosides with two or more glucose units and dextran es ters with a degree of substitution of 0.1 or less may be applied. The determination of the CMC of alkylpolyglycosides by solubilization of f luorescent substances shows a plot, typical for monomeric surfactants. The dextran esters show no CMC. They actually are polymeric surfactan ts and form monomolecular micelles. The differences in hemolytic activ ity of the alkylpolyglycosides run up to the factor 100. The hemolytic activity increases in this class of surfactants with the elongation o f the alkyl chain and decreases with increasing degree of glycosylatio n. It doesn't exist any correlation between the CMC and the hemolytic activity. For diazepam the differences in solubilization behaviour are rather low. The solubilization behaviour is more effective than that of Solutol(R) HS 15. The hemolytic activity of the dextran fatty ester s is low, compared with the alkylpolyglycosides.