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关于配体脂质体作为硼中子俘获疗法递送剂的初步实验。

Introductory experiments on ligand liposomes as delivery agents for boron neutron capture therapy.

作者信息

Bohl Kullberg Erika, Carlsson Jörgen, Edwards Katarina, Capala Jacek, Sjöberg Stefan, Gedda Lars

机构信息

Division of Biomedical Radiation Sciences, Rudbeck Laboratory, Uppsala University, 75185 Uppsala, Sweden.

出版信息

Int J Oncol. 2003 Aug;23(2):461-7.

Abstract

Liposomes are, when coupled to receptor ligands, candidates for receptor mediated delivery of boron for tumour therapy since they have capacity to deliver large amounts of boron per receptor interaction. With EGF-liposomes we present a pegylated ligand liposome delivery vehicle, containing water soluble boronated phenanthridine, WSP1, or water soluble boronated acridine, WSA1, for EGFR targeting. In the case of WSA1 a ligand dependent uptake was obtained and the boron uptake was as good as if free WSA1 was given. No ligand dependent boron uptake was seen for WSP1 containing liposomes. Thus, WSA1 is a candidate for further studies. Approximately 10(5) boron atoms were in each liposome. A critical assessment indicates that after optimization up to 10(6) boron atoms can be loaded. Since it is known that, for therapeutic effect, approximately 10(8)-10(9) boron atoms are needed in a single tumour cell it is realized that 10(2)-10(3) receptor interactions are needed to meet the demand. Tests applying cultured glioma cells indicate, without optimization of the delivery conditions, a boron uptake in the ppm range, which is necessary for successful BNCT. Thus, it seems possible to kill micro-invasive tumour cells with targeted liposomes if the delivery conditions are optimal.

摘要

脂质体与受体配体偶联后,是用于肿瘤治疗的受体介导硼递送的候选物,因为它们能够在每次受体相互作用时递送大量硼。通过表皮生长因子(EGF)脂质体,我们展示了一种聚乙二醇化的配体脂质体递送载体,其含有用于靶向表皮生长因子受体(EGFR)的水溶性硼化菲啶WSP1或水溶性硼化吖啶WSA1。对于WSA1,获得了依赖配体的摄取,并且硼摄取与给予游离WSA1时一样好。对于含WSP1的脂质体,未观察到依赖配体的硼摄取。因此,WSA1是进一步研究的候选物。每个脂质体中约有10⁵个硼原子。一项关键评估表明,优化后最多可负载10⁶个硼原子。由于已知对于治疗效果,单个肿瘤细胞中大约需要10⁸ - 10⁹个硼原子,所以意识到需要10² - 10³次受体相互作用才能满足需求。应用培养的胶质瘤细胞进行的测试表明,在未优化递送条件的情况下,硼摄取量在百万分之一的范围内,这对于成功的硼中子俘获疗法(BNCT)是必要的。因此,如果递送条件最佳,似乎有可能用靶向脂质体杀死微侵袭性肿瘤细胞。

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