64Cu Core-Labeled Nanoparticles with High Specific Activity via Metal-Free Click Chemistry

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• 作者：Dexing Zeng ; Nam S. Lee ; Yongjian Liu ; Dong Zhou ; Carmen S. Dence ; Karen L. Wooley ; John A. Katzenellenbogen ; Michael J. Welch
• 刊名：ACS Nano
• 出版年：2012
• 出版时间：June 26, 2012
• 年：2012
• 卷：6
• 期：6
• 页码：5209-5219
• 全文大小：677K
• 年卷期：v.6,no.6(June 26, 2012)
• ISSN：1936-086X

文摘

A novel strategy based on metal-free 鈥渃lick鈥?chemistry was developed for the copper-64 radiolabeling of the core in shell-cross-linked nanoparticles (SCK-NPs). Compared with Cu(I)-catalyzed click chemistry, this metal-free strategy provides the following advantages for Cu-64 labeling of the core of SCK-NPs: (1) elimination of copper exchange between nonradioactive Cu in the catalyst and DOTA-chelated Cu-64; (2) elimination of the internal click reactions between the azide and acetylene groups in the same NPs; and (3) increased efficiency of the click reaction because water-soluble Cu(I) does not need to reach the hydrophobic core of the NPs. When 50 mCi Cu-64 was used for the radiolabeling, the specific activity of the radiolabeled product was 975 Ci/渭mol at the end of synthesis, which represents the attachment of ca. 500 Cu-64 atoms per SCK-NP, giving in essence a 500-fold amplification of specific activity of the NP over that of the Cu-64 chelate. To the best of our knowledge, this is the highest specific activity obtained for Cu-64-labeled nanoparticles.

Keywords:

copper-64 radiolabeling; shell-cross-linked nanoparticles; high specific activity; specific activity amplification; metal-free click chemistry