Fluorescence imaging is a promising method widely used for the evaluation of the biodistribution and accumulation of various fluorescent agents cross-linked to the drug for effective therapy control. This work presents the methods for the functionalization of nanomaterials to provide them with fluorescent properties. The first of these methods is a unique technology for producing porous silicon with fluorescent properties. The second approach demonstrates linking of the fluorophores to inorganic nanoparticles (NP) using a spacer molecule ending with a functional group. For all these examples of fluorophores, biodistribution studies were performed with the fluorescent imaging system IVIS Lumina LT III (PerkinElmer, USA). It was noted that the size of particles and the method of their injection affect the distribution and accumulation in organs. The resulting materials can be used to develop platforms for theranostics.