Granisetron, a drug commonly used to prevent chemotherapy-induced nausea and vomiting, is difficult to administer due to its low oral bioavailability and potential side effects. Transdermal drug delivery offers a promising alternative to overcome these limitations. Liposomes, spherical lipid vesicles capable of encapsulating both hydrophilic and lipophilic drugs, have proven to be efficient vectors for transdermal delivery. This comprehensive review focuses on potential liposomes as vehicles for the transdermal delivery of Granisetron. Various liposome formulation techniques such as hydration and thin film sonication and their impact on the size, efficiency, and stability of liposome encapsulation are discussed. In addition, strategies to improve penetration will be explored, including the use of chemical and physical methods to improve skin penetration. In vitro and in vivo evaluations of liposomal Granisetron administration, including drug release kinetics, skin penetration studies, and therapeutic efficacy are summarized. In addition, the safety and biocompatibility aspects of liposomes as well as strategies to minimize potential toxicity and skin irritation are discussed. In addition, a comparison with other delivery systems such as oral tablets and intravenous infusion was performed to highlight the advantages and limitations of transdermal liposomal delivery. Future prospects and challenges associated with the administration of liposomal Granisetron are discussed, including the search for new lipid formulations and the need for clinical trials to demonstrate efficacy and safety. Overall, liposomes are proving to be effective vehicles for the transdermal delivery of Granisetron, offering improved bioavailability, fewer side effects, and better patient compliance.