Cancer is one of the most formidable global health challenges, needing ongoing progress in therapeutic approaches. Conventional cancer treatments, such as chemotherapy, frequently suffer from low solubility, systemic toxicity, and a lack of tailored drug delivery, resulting in unwanted side effects and limited efficacy. Surfactant-based drug delivery systems have emerged as a viable method for increasing drug solubility, stability, and tailored transport to tumor locations. Surfactants, due to their amphiphilic character, play an important role in the development of various drug delivery systems, such as micelles, liposomes, nanoemulsions, and lipid-based nanoparticles, which improve drug bioavailability and therapeutic index. This article looks at the fundamental role of surfactants in drug administration, including their classification (ionic, nonionic, amphoteric, and zwitterionic) and self-assembly behavior in the formation of micellar, vesicular, and emulsified nanocarriers. Various surfactant-based drug delivery platforms in oncology are explored, including polymeric and surfactant-stabilized micelles, liposomes (e.g., Doxil), nanoemulsions, solid lipid nanoparticles (SLNs), and nanostructured lipid carriers (NLCs). Furthermore, the use of surfactant-metal complexes in cancer therapy is emphasized because of their potential to improve therapeutic activity and selectivity. The review also looks at surfactant-enhanced drug targeting strategies, such as passive targeting using the enhanced permeability and retention (EPR) effect, active targeting with ligand-functionalized surfactant-based carriers, and stimuli-responsive systems designed for controlled drug release in the tumor microenvironment. Surfactant-based drug delivery advancements are explored, with an emphasis on current advances such as biodegradable and bio-inspired surfactants, combination therapies using surfactant-stabilized carriers, and AI-driven drug formulation techniques. Despite its potential, surfactant-based drug delivery systems confront several hurdles, including biocompatibility concerns, synthetic surfactant toxicity, stability issues, and scaling restrictions in pharmaceutical manufacture. Furthermore, regulatory barriers in clinical translation remain severe. Addressing these problems with innovative surfactant formulations, green chemical techniques, and sophisticated nanotechnological alterations will be critical to optimizing these systems for clinical use. This review provides a comprehensive analysis of the progress, challenges, and future perspectives of surfactant-based drug delivery systems in cancer therapy, highlighting their potential to revolutionize oncology treatments by improving drug efficacy, reducing systemic toxicity, and enabling precision medicine.