Characterization of the physicochemical properties of micelles composed of the novel platelet activating factor receptor antagonist, E5880 in an aqueous environment.
E5880, a novel platelet activating factor (PAF) receptor antagonist, was dispersed in water for use in 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 containing 49 molecules. The diameter of the micelle 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 (STAC) and cetyltrimethylammonium chloride (CTAC).
Asai
Yasuyuki
Y
Formulation Research Laboratory, Kawashima, Eisai Co., Ltd., 1 Takehaya-machi, Kawashima-cho, Hashima-gun, 501-6195 Gifu, Japan. y2-asai@hhc.eisai.co.jp
D008823:Micelles; D015394:Molecular Structure; D010316:Particle Size; D010880:Piperidines / Q000737:chemistry*; D010980:Platelet Membrane Glycoproteins / Q000037:antagonists & inhibitors*; D011726:Pyridinium Compounds / Q000737:chemistry*; D043562:Receptors, G-Protein-Coupled / Q000037:antagonists & inhibitors*; D012996:Solutions; D013500:Surface Tension
D008823:Micelles; D010880:Piperidines; D010980:Platelet Membrane Glycoproteins; D011726:Pyridinium Compounds; D043562:Receptors, G-Protein-Coupled; D012996:Solutions; C039351:platelet activating factor receptor; C072429:E 5880