The invention discloses a small molecule material (please see the structure in the description) used for anti-tumor drug delivery, a preparation method thereof and medicine-carrying application of the small molecule material. The small molecule material is prepared from two molecule carboxylation D-gluconic acid-delta-lactone and diamine which is connected with two molecule carboxylation D-gluconic acid-delta-lactone through a peptide bond. The small molecule material is used for delivering paclitaxel, doxorubicin, camptothecin and other anti-tumor drugs, prodrugs which are formed by bonding the small molecule material and the drugs can form nano-micelles in a self-assembly mode, in this way, the water solubility and biocompatibility of the drugs are improved, passive targeting is achieved under a tumor EPR effect, and the treatment effect and bioavailability of the drugs are improved.