This review explores the advancements and challenges in targeted drug delivery for breast cancer, a significant global health issue. Current treatments, including surgery, chemotherapy, radiation therapy, and targeted therapies, have improved patient outcomes but still face limitations such as adverse effects and drug resistance. The review highlights the potential of nanotechnology, particularly inorganic and organic nanoparticles, to selectively deliver therapeutic agents to tumor sites, enhancing drug efficacy and reducing side effects. It discusses various targeting strategies, including passive targeting through the enhanced permeability and retention (EPR) effect, active targeting using ligands and antibodies, and stimuli-responsive drug delivery systems. The review also examines different types of targeted drug delivery systems, such as nanoparticle-based systems, liposomal formulations, antibody-drug conjugates (ADCs), and polymer-based carriers, each with unique advantages and applications. Preclinical studies and clinical trials are discussed, showcasing the progress and challenges in translating these technologies into clinical practice. Finally, the review addresses future directions, including overcoming biological barriers, biodegradation and clearance of nanocarriers, and immunological considerations to improve the efficacy and safety of targeted drug delivery in breast cancer treatment.This review explores the advancements and challenges in targeted drug delivery for breast cancer, a significant global health issue. Current treatments, including surgery, chemotherapy, radiation therapy, and targeted therapies, have improved patient outcomes but still face limitations such as adverse effects and drug resistance. The review highlights the potential of nanotechnology, particularly inorganic and organic nanoparticles, to selectively deliver therapeutic agents to tumor sites, enhancing drug efficacy and reducing side effects. It discusses various targeting strategies, including passive targeting through the enhanced permeability and retention (EPR) effect, active targeting using ligands and antibodies, and stimuli-responsive drug delivery systems. The review also examines different types of targeted drug delivery systems, such as nanoparticle-based systems, liposomal formulations, antibody-drug conjugates (ADCs), and polymer-based carriers, each with unique advantages and applications. Preclinical studies and clinical trials are discussed, showcasing the progress and challenges in translating these technologies into clinical practice. Finally, the review addresses future directions, including overcoming biological barriers, biodegradation and clearance of nanocarriers, and immunological considerations to improve the efficacy and safety of targeted drug delivery in breast cancer treatment.