Formation of spherical micelles composed of the novel platelet activating factor receptor antagonist, E5880.
E5880, a novel platelet activating factor receptor antagonist, was dispersed in water for use in an injectable formulation and the physicochemical properties of the preparation were characterized. The critical concentration for formation of micelles was 0.12 mM. Using area per molecule data, the critical packing parameter was calculated, indicating that the structure of the micelles was spherical and that each micelle containes 49 molecules. The diameter of the micelles was 8.1 nm. Attractive interactions occurred between E5880 molecules in the micelle. The hydrocarbon region in the micelle was more rigid and less hydrated than that of other surfactants, stearyltrimethylammonium chloride and cetyltrimethylammonium chloride.
Asai
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Formulation Research Laboratory, Kawashima, Eisai Co., Ltd., Gifu, Japan. y2-asai@hhc.eisai.co.jp
D000465:Algorithms; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical; D002627:Chemistry, Physical; D008055:Lipids / Q000737:chemistry; D008823:Micelles; D010316:Particle Size; D010880:Piperidines / Q000737:chemistry*; D010972:Platelet Activating Factor / Q000037:antagonists & inhibitors*; D011726:Pyridinium Compounds / Q000737:chemistry*; D013499:Surface Properties
D008055:Lipids; D008823:Micelles; D010880:Piperidines; D010972:Platelet Activating Factor; D011726:Pyridinium Compounds; C072429:E 5880