Blume G, Cevc G, Crommelin M D, Bakker-Woudenberg I A, Kluft C, Storm G
Urologische Klinik und Poliklinik, Technischen Universität München, Germany.
Biochim Biophys Acta. 1993 Jun 18;1149(1):180-4. doi: 10.1016/0005-2736(93)90039-3.
One possibility for bringing drugs to their specific targets is to use the drug-laden liposomes that have been made target-specific by the attachment of appropriate proteins. Such 'directed' proteoliposomes and most other particles are rapidly removed from the bloodstream, however, by the mononuclear phagocytes in the liver and spleen. This causes suboptimal drug accumulation at the target site. Coating the liposome surface with poly(ethylene glycol) (PEG) may prolong the circulation time of liposomes. Using plasminogen as a homing device we have shown that the PEG-modified liposomes with such a homing device coupled to the ends of the long PEG chains may combine long vesicle circulation times in the blood with high target binding capability. The PEG-coated proteoliposomes with homing devices attached at the very bilayer surface, on the contrary, are longlived but have only little or no capability to bind to their targets.
将药物输送到其特定靶点的一种可能性是使用载有药物的脂质体，这些脂质体通过附着适当的蛋白质而具有靶向特异性。然而，这种“定向”蛋白脂质体和大多数其他颗粒会被肝脏和脾脏中的单核吞噬细胞迅速从血液中清除。这导致药物在靶点部位的积累不理想。用聚乙二醇（PEG）包被脂质体表面可能会延长脂质体的循环时间。我们已经表明，使用纤溶酶原作为归巢装置，将这种归巢装置连接到长PEG链末端的PEG修饰脂质体可以在血液中实现长循环时间与高靶向结合能力的结合。相反，在双层表面附着归巢装置的PEG包被蛋白脂质体寿命长，但与靶点结合的能力很小或没有。
