Gedda Lars, Edwards Katarina
Department of Radiology, Oncology and Radiation Sciences, Unit of Biomedical Radiation Sciences, Rudbeck Laboratory, Uppsala University, 751 85 Uppsala, Sweden.
Tumour Biol. 2012 Jun;33(3):661-7. doi: 10.1007/s13277-012-0341-3.
The Nuclisome concept builds on a novel two-step targeting strategy with the aim to deliver short-range Auger-electron-emitting radionuclides to nuclear DNA of tumor cells. The concept is based on the use of Nuclisome-particles, i.e., tumor-targeted PEG-stabilized liposomes loaded with a unique DNA-intercalating compound that enables specific and effective delivery of radionuclides to DNA. The specific and potent two-step targeting leads to eradication of tumor cells while toxicity to normal organs is reduced to a minimum. Results of in vitro and in vivo studies point towards the Nuclisome concept as a promising strategy for the treatment of small tumor masses and, in particular, for the elimination of spread single cells and micrometastases.
核小体概念基于一种新颖的两步靶向策略,旨在将发射俄歇电子的短程放射性核素递送至肿瘤细胞的核DNA。该概念基于核小体颗粒的使用,即负载有独特DNA嵌入化合物的肿瘤靶向聚乙二醇稳定脂质体,该化合物能够将放射性核素特异性且有效地递送至DNA。这种特异性且强效的两步靶向可导致肿瘤细胞的根除,同时将对正常器官的毒性降至最低。体外和体内研究结果表明,核小体概念是治疗小肿瘤块,特别是消除扩散的单个细胞和微转移的一种有前景的策略。