The article reviews the advancements in folate receptor-mediated transporters for cancer therapy and diagnosis. It highlights the challenges of traditional chemotherapy and the potential of targeted drug delivery systems, particularly those utilizing cell membrane receptors like the folate receptor. The review discusses the development of targeted nanocarriers and small molecule-drug conjugates (SMDCs) that can deliver drugs specifically to malignant cells, reducing side effects and improving treatment efficacy. The focus is on the structural design, loading, and release chemistry of these drug transporters, emphasizing the importance of linkers and spacers in controlling drug release and stability. The article also explores the role of folate receptors in cancer, particularly in brain and breast cancers, and the use of folic acid-conjugated drug transporters to overcome biological barriers. The review provides a comprehensive overview of the current state of research and the potential of these targeted delivery systems in cancer treatment and diagnosis.The article reviews the advancements in folate receptor-mediated transporters for cancer therapy and diagnosis. It highlights the challenges of traditional chemotherapy and the potential of targeted drug delivery systems, particularly those utilizing cell membrane receptors like the folate receptor. The review discusses the development of targeted nanocarriers and small molecule-drug conjugates (SMDCs) that can deliver drugs specifically to malignant cells, reducing side effects and improving treatment efficacy. The focus is on the structural design, loading, and release chemistry of these drug transporters, emphasizing the importance of linkers and spacers in controlling drug release and stability. The article also explores the role of folate receptors in cancer, particularly in brain and breast cancers, and the use of folic acid-conjugated drug transporters to overcome biological barriers. The review provides a comprehensive overview of the current state of research and the potential of these targeted delivery systems in cancer treatment and diagnosis.