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. 1999 Apr 27;96(9):5182-7.
doi: 10.1073/pnas.96.9.5182.

In vivo studies of fullerene-based materials using endohedral metallofullerene radiotracers

D W Cagle  1 , S J Kennel, S Mirzadeh, J M Alford, L J Wilson
Affiliations

In vivo studies of fullerene-based materials using endohedral metallofullerene radiotracers

D W Cagle et al. Proc Natl Acad Sci U S A. .

Abstract

Biodistribution studies of a water-soluble radioactive metallofullerene compound have been conducted using BALB/c mice. To this end, a sample containing Hox@C82 (x = 1, 2) was purified and derivatized to prepare the water-soluble metallofullerol, Hox@C82(OH)y. This metallofullerol was then neutron-activated (165Ho[n,gamma]166Ho) to prepare the 166Hox@C82(OH)y analog as a radiotracer, which was monitored, after intravenous administration, for up to 48 hours by using dissection radioanalysis, and its biodistribution was compared with a control compound, Na2[166Ho(DTPA)(H2O)]. Results showed selective localization of the 166Hox@C82(OH)y tracer in the liver but with slow clearance, as well as uptake by bone without clearance. In contrast, excretion of the control compound was nearly quantitative after 1 hour. The fate of 166Ho was also explored by a metabolism study of 166Hox@C82(OH)y in Fischer rats. Results indicated 20% excretion of intact 166Hox@C82(OH)y within 5 days. The present findings demonstrate the feasibility of using water-solubilized metallofullerene radiotracers to monitor the fate of fullerene-based materials in animals, and suggest that water-solubilized fullerene materials, in general, may be useful components in drug design.

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Figures

Figure 1
Figure 1
HPLC Separation of o-xylene-soluble high-temperature holmium metallofullerene sublimate from a Buckyprep column under anaerobic conditions (flow rate of 8 ml⋅min−1, retention time (Hox@C82) = 5.8–6.4 min, 305 nm).
Figure 2
Figure 2
LD-TOF MS Data of the HPLC-purified fraction containing Hox@C82 (x = 1, 2).
Figure 3
Figure 3
Biodistribution of Na2[166Ho(DTPA)(H2O)] injected intravenously in 200 μl of Mes buffer into BALB/c Mice. The animals were sacrificed, and organs were sampled at 1, 4, 24, and 48 h, followed by measurement of the 166Ho 80.5 KeV γ-emission. Three animals were assayed at each time point, and reported values are the average of the % ID per g of tissue (σ range: 0.14–0.60% ID per g).
Figure 4
Figure 4
Biodistribution of 166Hox@C82(OH)y in BALB/c mice at 1, 4, 24, and 48 h after injection. Conditions and details are the same as for Fig. 3 [σ range: 0.32–5.69% ID per g (liver and spleen) and 0.03–1.23% ID per g (other tissue)].
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