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目的制备壳寡糖-硬脂酸(COS-SA)及具有肝靶向性的甘草次酸-壳寡糖-硬脂酸(GA-COS-SA)药物载体,并研究其形成胶束的理化性质。方法采用碳二亚胺作为偶联剂,使硬脂酸、甘草次酸先后与壳寡糖中氨基发生取代反应,制得两种壳寡糖嫁接聚合物。采用超声方法制备二者的胶束溶液,染料增溶法测定二者的临界胶束浓度(CMC),激光光散射仪测定胶束的粒径,透射电镜观察胶束的形态。结果成功制得两种壳寡糖聚合物,所形成的胶束具有较低的CMC,胶束粒子呈较规则的球形,粒径分别为250、228 nm,且随疏水链段取代度增加,粒径变小,CMC降低。结论胶束具有较好的物理化学性质,是具有发展前景的药物载体。
OBJECTIVE To prepare chitooligosaccharides-stearic acid (COS-SA) and liver-targeting glycyrrhetinic acid-chitosan-stearic acid (GA-COS-SA) nature. Methods Carbodiimide was used as the coupling agent to make the substitution reactions of stearic acid and glycyrrhetinic acid with the amino groups in chitooligosaccharides. Two kinds of chitooligosaccharides graft polymers were prepared. The micellar solutions of the two micelles were prepared by ultrasonic method. The critical micelle concentration (CMC) of the two micelles was determined by dye solubilization method. The size of micelles was determined by laser light scattering and the morphology of micelles was observed by transmission electron microscopy. Results Two chitooligosaccharides polymers were obtained successfully. The formed micelles had low CMC and micellar particles with regular spherical shape with diameter of 250 and 228 nm, respectively. With the increase of the degree of substitution, The particle size becomes smaller and CMC decreases. Conclusion Micelles have good physico-chemical properties and are promising drug carriers.