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A procedure for dispersing oxidized single-wall carbon nanohorns (oxSWNHs) in aqueous solution using a polyethylene glycol-doxorubicin (PEG-DXR) conjugate is described. In this procedure, oxSWNHs were first incubated with PEG-DXR in dimethyl sulfoxide (DMSO) or N,N-dimethylformamide (DMF), two organic solvents with relatively high electric dipole moments, after which the solvent was gradually changed to an aqueous one via addition of water until the final concentration of DMSO or DMF reached 10%. The PEG-DXR-oxSWNH complex that was obtained was able to pass through dextran-based chromatographic media (Sephadex G25) equilibrated with water. By contrast, untreated oxSWNHs and DXR-treated or PEG-treated oxSWNHs were unable to penetrate the column, indicating that the PEG-DXR conjugate endowed oxSWNHs with dispersibility in aqueous solution. In gel filtration experiments, the presence of free DXR had an inhibitory effect on the penetrability of PEG-DXR-oxSWNH complexes, which is consistent with the idea that PEG-DXR interacts with the surfaces of oxSWNHs via its DXR moiety. Quantitative analyses showed that the complex contained more than 250 mg of PEG-DXR for each gram of oxSWNHs. The average diameter of the dispersed complex was estimated to be approximately 160 nm using dynamic light scattering analysis. These results suggest that our method has the potential to open the way for the use of oxSWNHs as a clinically practical drug carrier.
Murakami et al. (Fri,) studied this question.