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Cyclodextrin derivatives conjugated with one or more saccharide moieties are expected to be useful as targeted drug-delivery systems. We prepared a cyclodextrin conjugated with two arbutin moieties, which was designed as a model for a drug carrier having a high ability for the inclusion of the anticancer agent doxorubicin. Studies using a surface plasmon resonance optical biosensor showed that the cyclodextrin derivative has an extremely high association constant of 1.4 ' 10 8 M-1 for immobilized doxorubicin.