Dunnick J K, McDougall I R, Aragon S, Goris M L, Kriss J P
J Nucl Med. 1975 Jun;16(6):483-7.
Artificial spherules or vesicles of 900 A in diameter formed from phosphatidylcholine and gangliosides and enclosing 99mTcO4 - (standard preparation) survive intact in the circulation of the mouse. Polyamino acids and protein have been incorporated into and onto the vesicles; such vesicles remain intact as determined by diffusion dialysis studies and by electron paramagnetic resonance studies of vesicles enclosing spin label. In studying the distribution of polyamino acid-vesicles and protein vesicles in vivo, it was found that the latter distribute differently from standard vesicles or free protein alone whereas aromatic polyamino acid-vesicles concentrate in the liver and spleen to a greater extent than standard vesicles. We conclude that the permeability and stability characteristics of vesicles may be preserved when they are modified by the addition of protein or polyamino acids and that such modification of vesicles may be associated with an alteration of their fate in vivo. The potential exists to use vesicles as carriers of radiopharmaceuticals and other drugs and to direct the vesicles preferentially to tissue targets in vivo.
由磷脂酰胆碱和神经节苷脂形成的、直径为900埃的人工小球或囊泡,包裹着高锝酸盐(标准制剂),在小鼠循环系统中能完整存活。聚氨基酸和蛋白质已被整合到囊泡内部及表面;通过扩散透析研究以及对包裹自旋标记物的囊泡进行电子顺磁共振研究表明,此类囊泡保持完整。在研究聚氨基酸囊泡和蛋白质囊泡在体内的分布时发现,后者的分布与标准囊泡或单独的游离蛋白质不同,而芳香族聚氨基酸囊泡比标准囊泡更易在肝脏和脾脏中聚集。我们得出结论,当囊泡通过添加蛋白质或聚氨基酸进行修饰时,其通透性和稳定性特征可能得以保留,并且这种囊泡修饰可能与其在体内的命运改变有关。利用囊泡作为放射性药物和其他药物的载体,并在体内将囊泡优先导向组织靶点具有潜力。