Halbert G W, Stuart J F, Florence A T
Cancer Chemother Pharmacol. 1985;15(3):223-7. doi: 10.1007/BF00263890.
Low-density lipoprotein particles are potential drug carriers, but only lipophilic drug species partition into the core of the system. In this paper the polar drug methotrexate has been coupled to the exterior protein of low density lipoprotein (LDL) particles using the reagent 1-ethyl-3(3'-dimethylaminopropyl) carbodiimide HCl. The coupled system was sized by photon correlation spectroscopy and the in vitro activity of the complex determined against L1210 cells maintained in medium supplemented with fetal calf serum. The reaction between methotrexate and low density lipoprotein is variable but quantifiable, about ten drug molecules being attached to each LDL particle, resulting in an increase in the radius and polydispersity of the particles. The activity of the complex against L1210 murine leukaemia cells has been demonstrated in vitro, but it is 30 times less active than free drug.
低密度脂蛋白颗粒是潜在的药物载体，但只有亲脂性药物种类会分配到该体系的核心部位。在本文中，使用试剂盐酸1-乙基-3-(3'-二甲氨基丙基)碳二亚胺，将极性药物甲氨蝶呤偶联到低密度脂蛋白（LDL）颗粒的外部蛋白质上。通过光子相关光谱法对偶联体系进行了大小测定，并针对在补充有胎牛血清的培养基中培养的L1210细胞测定了该复合物的体外活性。甲氨蝶呤与低密度脂蛋白之间的反应是可变的，但可定量，每个LDL颗粒约附着十个药物分子，导致颗粒半径和多分散性增加。该复合物对L1210小鼠白血病细胞的活性已在体外得到证实，但其活性比游离药物低30倍。
