Torchilin V P, Smirnov V N
Ukr Biokhim Zh (1978). 1984 May-Jun;56(3):339-45.
Liposomes are considered to be one of the perspective carriers for drug targeting in the organism. The drug preparation can be incorporated into the inner water space of liposomes and the molecule capable of recognition and binding to the target-zone should be bound to the outer surface of the membrane. Thus, the elaboration of effective methods for binding affinity proteins with liposome surface is of particular importance. Two principal schemes of such a binding are worked out: introduction of reactive groups into the liposome membrane with subsequent chemical protein binding or preliminary modification of protein by the hydrophobic reagent with its subsequent noncovalent incorporation into the liposome. In the first case liposomes can contain reactive aminophospholipids, dithiopropionate-phospholipids and fatty acid derivatives of polysaccharides activated by oxidation. Enzymes and antibodies are bound to liposomes, preserving the specific activity, with the binding yield up to 40% and the bound protein quantity of about 2 X 10(-4) mol per mol of lipid. In the second case proteins modified by fatty acid derivatives or by phosphatydyl inositol are incorporated into liposomes in quantity of about 2 X 10(-3) mol per mol of lipid and with binding yield of about 50%.
脂质体被认为是生物体内药物靶向的有前景的载体之一。药物制剂可被包裹在脂质体的内部水相中，而能够识别并结合靶区的分子应结合在膜的外表面。因此，开发将亲和蛋白与脂质体表面结合的有效方法尤为重要。已经设计出两种主要的结合方案：在脂质体膜中引入反应基团，随后进行蛋白质化学结合；或者先用疏水试剂对蛋白质进行初步修饰，然后将其非共价掺入脂质体中。在第一种情况下，脂质体可含有反应性氨基磷脂、二硫代丙酸磷脂以及经氧化激活的多糖脂肪酸衍生物。酶和抗体与脂质体结合后，仍保留其比活性，结合产率高达40%，每摩尔脂质结合的蛋白量约为2×10⁻⁴摩尔。在第二种情况下，经脂肪酸衍生物或磷脂酰肌醇修饰的蛋白质以每摩尔脂质约2×10⁻³摩尔的量掺入脂质体中，结合产率约为50%。
