[The hemolysis and solubilization behavior of nonionic polymer surface-active agents classes]. 1995

T Reinhart, and K H Bauer
Lehrstuhl für Pharmazeutische Technologie, Albert-Ludwigs-Universität, Freiburg/Brsg.

The solubilization of poorly water soluble drugs in surfactant solutions is still a problem in pharmaceutical technology. There doesn't exist any surfactant which can be applied unrestricted in parenteral dosage forms. For this reason, alkylpolyglycosides and fatty esters of dextran were investigated. Their solubilization behaviour and hemolytic activity was tested and compared to established surfactants. For solubilization, only water soluble surfactants can be used. That means, that only alkylpolyglycosides with two or more glucose units and dextran esters with a degree of substitution of 0.1 or less may be applied. The determination of the CMC of alkylpolyglycosides by solubilization of fluorescent substances shows a plot, typical for monomeric surfactants. The dextran esters show no CMC. They actually are polymeric surfactants and form monomolecular micelles. The differences in hemolytic activity of the alkylpolyglycosides run up to the factor 100. The hemolytic activity increase in this class of surfactants with the elongation of the alkyl chain and decreases with increasing degree of glycosylation. 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 HS 15. The hemolytic activity of the dextran fatty esters is low, compared with the alkylpolyglycosides.

UI MeSH Term Description Entries
D008823 Micelles Particles consisting of aggregates of molecules held loosely together by secondary bonds. The surface of micelles are usually comprised of amphiphatic compounds that are oriented in a way that minimizes the energy of interaction between the micelle and its environment. Liquids that contain large numbers of suspended micelles are referred to as EMULSIONS. Micelle
D002627 Chemistry, Physical The study of CHEMICAL PHENOMENA and processes in terms of the underlying PHYSICAL PHENOMENA and processes. Physical Chemistry,Chemistries, Physical,Physical Chemistries
D003911 Dextrans A group of glucose polymers made by certain bacteria. Dextrans are used therapeutically as plasma volume expanders and anticoagulants. They are also commonly used in biological experimentation and in industry for a wide variety of purposes. Dextran,Dextran 40,Dextran 40000,Dextran 70,Dextran 75,Dextran 80,Dextran B-1355,Dextran B-1355-S,Dextran B1355,Dextran B512,Dextran Derivatives,Dextran M 70,Dextran T 70,Dextran T-40,Dextran T-500,Hemodex,Hyskon,Infukoll,Macrodex,Polyglucin,Promit,Rheodextran,Rheoisodex,Rheomacrodex,Rheopolyglucin,Rondex,Saviosol,Dextran B 1355,Dextran B 1355 S,Dextran T 40,Dextran T 500
D005453 Fluorescence The property of emitting radiation while being irradiated. The radiation emitted is usually of longer wavelength than that incident or absorbed, e.g., a substance can be irradiated with invisible radiation and emit visible light. X-ray fluorescence is used in diagnosis.
D006027 Glycosides Any compound that contains a constituent sugar, in which the hydroxyl group attached to the first carbon is substituted by an alcoholic, phenolic, or other group. They are named specifically for the sugar contained, such as glucoside (glucose), pentoside (pentose), fructoside (fructose), etc. Upon hydrolysis, a sugar and nonsugar component (aglycone) are formed. (From Dorland, 28th ed; From Miall's Dictionary of Chemistry, 5th ed) Glycoside
D006461 Hemolysis The destruction of ERYTHROCYTES by many different causal agents such as antibodies, bacteria, chemicals, temperature, and changes in tonicity. Haemolysis,Extravascular Hemolysis,Intravascular Hemolysis,Extravascular Hemolyses,Haemolyses,Hemolyses, Extravascular,Hemolyses, Intravascular,Hemolysis, Extravascular,Hemolysis, Intravascular,Intravascular Hemolyses
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D013050 Spectrometry, Fluorescence Measurement of the intensity and quality of fluorescence. Fluorescence Spectrophotometry,Fluorescence Spectroscopy,Spectrofluorometry,Fluorescence Spectrometry,Spectrophotometry, Fluorescence,Spectroscopy, Fluorescence
D013501 Surface-Active Agents Agents that modify interfacial tension of water; usually substances that have one lipophilic and one hydrophilic group in the molecule; includes soaps, detergents, emulsifiers, dispersing and wetting agents, and several groups of antiseptics. Surface Active Agent,Surface-Active Agent,Surfactant,Surfactants,Tenside,Amphiphilic Agents,Surface Active Agents,Tensides,Active Agent, Surface,Active Agents, Surface,Agent, Surface Active,Agent, Surface-Active,Agents, Amphiphilic,Agents, Surface Active,Agents, Surface-Active
D055598 Chemical Phenomena The composition, structure, conformation, and properties of atoms and molecules, and their reaction and interaction processes. Chemical Concepts,Chemical Processes,Physical Chemistry Concepts,Physical Chemistry Processes,Physicochemical Concepts,Physicochemical Phenomena,Physicochemical Processes,Chemical Phenomenon,Chemical Process,Physical Chemistry Phenomena,Physical Chemistry Process,Physicochemical Phenomenon,Physicochemical Process,Chemical Concept,Chemistry Process, Physical,Chemistry Processes, Physical,Concept, Chemical,Concept, Physical Chemistry,Concept, Physicochemical,Concepts, Chemical,Concepts, Physical Chemistry,Concepts, Physicochemical,Phenomena, Chemical,Phenomena, Physical Chemistry,Phenomena, Physicochemical,Phenomenon, Chemical,Phenomenon, Physicochemical,Physical Chemistry Concept,Physicochemical Concept,Process, Chemical,Process, Physical Chemistry,Process, Physicochemical,Processes, Chemical,Processes, Physical Chemistry,Processes, Physicochemical

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