Formation of spherical micelles by the novel platelet activating factor receptor antagonist, E5880.
E5880, a novel platelet activating factor receptor antagonist, was dispersed in water for the preparation of injectable formulation and the physicochemical properties of the micelles were characterized. The critical concentration for formation of micelles was 0.12 mM. Using the area per molecule results, the critical packing parameter was calculated and showed that the structure was composed of spherical micelles and the number of the molecules per micelle was 88. The diameter of a micelle was 8.1 nm. The fluidity and micropolarity around the hydrocarbon region of the micelles were evaluated and compared to the surfactants, stearyltrimethylammmonium chloride and cetyltrimethylammonium chloride.
Formulation Research Laboratory, Kawashima, Eisai Co, Ltd, Hashima-gun, Gifu, Japan. t4-nomura@nnc.eisai.co.jp
T
T
Nomura
Y
Y
Asai
N
N
Murahashi
K
K
Iwamoto
D008055:Lipids / Q000737:chemistry; D008560:Membrane Fluidity; D008823:Micelles; D010316:Particle Size; D010880:Piperidines / Q000737:chemistry* / Q000494:pharmacology; D010980:Platelet Membrane Glycoproteins / Q000037:antagonists & inhibitors / Q000737:chemistry*; D011726:Pyridinium Compounds / Q000737:chemistry* / Q000494:pharmacology; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; D013500:Surface Tension
D008055:Lipids; D008823:Micelles; D010880:Piperidines; D010980:Platelet Membrane Glycoproteins; D011726:Pyridinium Compounds; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; C039351:platelet activating factor receptor; C072429:E 5880