The present invention provides hydrophilic bilirubin derivative particles containing a metal, a use thereof, and a preparation method therefor. The bilirubin derivative particles of the present invention form coordinate bonds with various metals, and thus can be used in MR diagnosis, CT diagnosis, photo-acoustic diagnosis, PET diagnosis, or optical diagnosis. The bilirubin derivative particles of the present invention can release an anticancer drug encapsulated therein to the outside by the combinaiton with a platinum-based anticancer drug and the degradation by a stimulation of light/reactive oxygen species, and exhibit antiinflammatory and anticancer activities, and thus the bilirubin derivative particles of the present invention have a concept of theranostics in which the bilirubin derivative particles can be for therapeutic uses as well as diagnositic uses. Furthermore, the bilirubin derivative particles of the present invention is reactive with reactive oxygen species, and thus can be used as a composition, sensor, kit, contrast agent, or device for detecting the kind and concentration of reactive oxygen species.
