Samokhin G P, Smirnov M D, Muzykantov V R, Domogatsky S P, Smirnov V N
J Appl Biochem. 1984 Feb-Apr;6(1-2):70-5.
The effect of bloodstream factors (flow rate and blood cellular elements) on the behavior of an experimental system simulating drug targeting to injured sites of vessel walls was studied. The system consisted of red blood cells carrying antibody to type I human collagen (drug carrier) and plastic tube with a collagen-coated inner surface (target). The tube was perfused with a 0.5% (v/v) suspension of 51Cr-labeled red blood cells at different linear flow rates and the red blood cell binding to the tube was determined by gamma-counting. It was demonstrated that an increase in the linear flow rate from 0 to 2 cm/s leads at first to increase of red blood cell binding from 2 X 10(5) to 7 X 10(5) cells/cm2 and then to the decrease of binding back to 2 X 10(5) cells/cm2. In the presence of 50% (v/v) of intact red blood cells the binding continuously increases from 2 X 10(5) to 2.5 X 10(6) cells/cm2 without a subsequent drop. On the basis of the obtained results it is concluded that the behavior of the systems for drug targeting in simple in vitro models can drastically differ from the conditions present in vivo.
研究了血流因素(流速和血细胞成分)对模拟药物靶向血管壁损伤部位的实验系统行为的影响。该系统由携带抗I型人胶原蛋白抗体的红细胞(药物载体)和内表面涂有胶原蛋白的塑料管(靶标)组成。以不同的线性流速用51Cr标记的红细胞的0.5%(v/v)悬浮液灌注该管,并通过γ计数测定红细胞与管的结合。结果表明,线性流速从0增加到2 cm/s时,首先导致红细胞结合从2×10⁵个细胞/cm²增加到7×10⁵个细胞/cm²,然后结合又降至2×10⁵个细胞/cm²。在存在50%(v/v)完整红细胞的情况下,结合持续从2×10⁵个细胞/cm²增加到2.5×10⁶个细胞/cm²,随后没有下降。根据所得结果得出结论,简单体外模型中药物靶向系统的行为可能与体内情况有很大不同。