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. 2010 Apr 14;132(14):4980-1.
doi: 10.1021/ja9093617.

Encapsulation of a radiolabeled cluster inside a fullerene cage, (177)Lu(x)Lu((3-x))N@C(80): an interleukin-13-conjugated radiolabeled metallofullerene platform

Michael D Shultz  1 , James C Duchamp, John D Wilson, Chun-Ying Shu, Jiechao Ge, Jianyuan Zhang, Harry W Gibson, Helen L Fillmore, Jerry I Hirsch, Harry C Dorn, Panos P Fatouros
Affiliations

Encapsulation of a radiolabeled cluster inside a fullerene cage, (177)Lu(x)Lu((3-x))N@C(80): an interleukin-13-conjugated radiolabeled metallofullerene platform

Michael D Shultz et al. J Am Chem Soc. .

Abstract

In this communication, we describe the successful encapsulation of (177)Lu into the endohedral metallofullerene (177)Lu(x)Lu(3-x)N@C(80) (x = 1-3) starting with (177)LuCl(3) in a modified quartz Kraschmer-Huffman electric generator. We demonstrate that the (177)Lu (beta-emitter) in this fullerene cage is not significantly released for a period of up to at least one-half-life (6.7 days). We also demonstrate that this agent can be conjugated with an interleukin-13 peptide that is designed to target an overexpressed receptor in glioblastoma multiforme tumors. This nanoparticle delivery platform provides flexibility for a wide range of radiotherapeutic and radiodiagnostic multimodal applications.

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Figures

Figure 1
Figure 1
Left: illustration of possible cage breakdown or retention due to β-decay events. Right: box plots corresponding to the control, aqueous and toluene extracts of 177LuxLu(3-x)N@C80 after 6.7 days.
Scheme 1
Scheme 1
Functionalization and conjugation of 177LuxLu(3-x)N@C80. with TAMRA labeled IL-13 peptide. Z = ~26, y = ~16, n = 1 or 2.
Figure 2
Figure 2
PAGE Images. From left to right: TAMRA labeled IL-13 peptide alone, visible lane; 177LuxLu(3-x)N@C80-TAMRA-IL-13 peptide lanes: visible, fluorescent and autoradiograph. Red rectangle shows the 177LuxLu(3-x)N@C80-TAMRA-IL-13 peptide conjugate.
See this image and copyright information in PMC

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