Klibanov A L, Muzykantov V R, Ivanov N N, Torchilin V P
Anal Biochem. 1985 Nov 1;150(2):251-7. doi: 10.1016/0003-2697(85)90507-x.
The model system for the analysis of targeted liposomes is proposed--the layer of protein antigen adsorbed on polystyrene wells. Antibodies were treated with palmitoyl chloride and liposomes were produced by the cholate dialysis method in the presence of the modified protein (7 X 10(-4) mol protein/mol lipid). Affinity of antibody-bearing liposomes to the antigen on the surface of Multiwell plates was studied, and apparent dissociation constant value was estimated: KD was in the range 1.5 to 5 X 10(-9) M liposomes. Sequential transfers of liposomes in antigen-coated plates revealed that the high-affinity fraction of liposomes is adsorbed first. The bound fraction has 1.7-times-higher protein content. For effective in vivo targeting it would be necessary to have high-affinity liposomes and a high concentration of the target antigen.
提出了用于分析靶向脂质体的模型系统——吸附在聚苯乙烯孔上的蛋白质抗原层。用棕榈酰氯处理抗体，并在修饰蛋白（7×10⁻⁴摩尔蛋白/摩尔脂质）存在的情况下通过胆酸盐透析法制备脂质体。研究了携带抗体的脂质体与多孔板表面抗原的亲和力，并估计了表观解离常数：脂质体的KD在1.5至5×10⁻⁹ M范围内。脂质体在抗原包被板中的连续转移表明，高亲和力部分的脂质体首先被吸附。结合部分的蛋白质含量高1.7倍。为了实现有效的体内靶向，需要有高亲和力的脂质体和高浓度的靶抗原。
