The biggest obstacles in treating cancer with traditional chemotherapy are unpleasant side effects and drug resistance. A growing amount of interest has been exhibited in using aptamers as target ligands for targeted cancer therapy and specific cancer cell identification due to their distinct benefits. Aptamer‐conjugated nano‐materials have recently provided new prospects in cancer treatment with their improved therapeutic efficacy and capability of reducing toxicity. Consequently, they are not perceived as alien substances our body, which allows their comfortable acceptance. Several tumor markers such as nucleolin, mucin, and the epidermal growth factor receptor can be effectively recognised by aptamers. In addition, glycoproteins on the surface of tumour cells can be recognised using aptamers. So surface modification of drug by aptamer are accomplished for enhanced tumor‐specific recognition by which drug‐ specific accretion, internalization, and drug retention in tumors increased through specific ligand‐mediated interactions and thus therapeutic index is increased. Here, we highlight some promising classes of aptamer‐conjugated nanoparticles for the specific recognition of cancer cells and targeted drug delivery and the molecular mechanism and immunomodulatory regulation of these aptamer have been focused.This article is protected by copyright. All rights reserved.