Kullberg Erika Bohl, Nestor Marika, Gedda Lars
Division of Biomedical Radiation Sciences, Department of Oncology, Radiology and Clinical Immunology, Rudbeck Laboratory, Uppsala University, S-751 85 Uppsala, Sweden.
Pharm Res. 2003 Feb;20(2):229-36. doi: 10.1023/a:1022223204460.
The aim of this work was to investigate the cellular binding and processing of polyethylene glycol-stabilized epidermal growth factor (EGF) liposomes. The liposomes were actively loaded with water-soluble boronated acridine (WSA), primarily developed for boron neutron capture therapy.
The uptake, internalization, and retention of EGF-liposome conjugates were studied in two cultured monolayer cell-lines, A-431 and U-343, with regard to the nuclide-label on the targeting agent, the carrier, and the load. The subcellular localization of WSA was studied using confocal microscopy.
We found that the liposome complex was internalized after specific binding to the EGF receptor. After internalization in the tumor cells, WSA was distributed mainly in the cytoplasm and was shown to have long cellular retention, with 80% of the boron remaining after 48 h.
The long retention of the compound and the cellular boron concentration reached makes these targeted liposomes interesting for further development toward boron neutron capture therapy.
本研究旨在探究聚乙二醇稳定化表皮生长因子（EGF）脂质体的细胞结合及处理情况。这些脂质体被主动装载了主要用于硼中子俘获疗法的水溶性硼化吖啶（WSA）。
针对靶向剂、载体及负载物上的核素标记，研究了EGF-脂质体偶联物在两种培养的单层细胞系A-431和U-343中的摄取、内化及保留情况。使用共聚焦显微镜研究了WSA的亚细胞定位。
我们发现脂质体复合物在与EGF受体特异性结合后被内化。在肿瘤细胞内化后，WSA主要分布在细胞质中，且显示出在细胞内的长时间保留，48小时后仍有80%的硼留存。
该化合物的长时间保留以及所达到的细胞硼浓度使得这些靶向脂质体在硼中子俘获疗法的进一步开发中具有吸引力。
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