Characterization of the physicochemical properties of the micelles by the novel platelet activating factor receptor antagonist E5880.
E5880, a novel platelet activating factor receptor antagonist, was dispersed in the buffer solution (4.8 mM citric acid, 10% lactose, pH 2.8) for the preparation of an injectable formulation and the physicochemical properties of the micelles were characterized. The critical micelle concentration of E5880 was 0.12 mM. Using the area per molecule results, the critical packing parameter was calculated and showed that the structure was spherical and the number of molecules in the aggregates was 46. The diameter of the micelle was 5.6 nm. The micropolarity around the hydrocarbon region of the micelle was similar to that of isobutanol.
Asai
Y
Y
Formulation Research Laboratory, Kawashima, Eisai Co. Ltd., Gifu, Japan.
Watanabe
S
S
D000465:Algorithms; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D008027:Light; D008823:Micelles; D008970:Molecular Weight; D010316:Particle Size; D010880:Piperidines / Q000737:chemistry*; D010972:Platelet Activating Factor / Q000037:antagonists & inhibitors*; D010980:Platelet Membrane Glycoproteins / Q000037:antagonists & inhibitors*; D011726:Pyridinium Compounds / Q000737:chemistry*; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; D012542:Scattering, Radiation; D013050:Spectrometry, Fluorescence; D013499:Surface Properties
D008823:Micelles; D010880:Piperidines; D010972:Platelet Activating Factor; D010980:Platelet Membrane Glycoproteins; D011726:Pyridinium Compounds; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; C039351:platelet activating factor receptor; C072429:E 5880