Traditional cancer pharmaceutical preparations suffer from many drawbacks, such as their nonselective damage to both tumor and normal cells, as well as their poor solubility and serious adverse effects affecting the patients’ productivity and quality of life. This chapter highlights the benefits of utilizing vesicular systems as carriers for medicines for cancer treatment. Liposomes and other vesicles (niosomes, bilosomes, ethosomes, tranethosomes, transfersomes, aspasomes, and other types) enable targeted drug delivery to tumor tissues, improving drug solubility, bioavailability, and efficacy while diminishing side effects. The focus of this chapter is to present an overview of different types of vesicles, their composition, methods of preparation, and advantages they can offer in the field of medicine. Some market products and formulations under clinical studies are listed. Also, the challenges faced and future prospects are discussed.