This chapter reviews the current progress in liposome based pharmaceuticals with particular emphasis on the carrier design, size, surface properties, drug delivery performances and therapeutic applications for different routes of administration. There were described selected examples of encapsulation of drug substances by liposomes which allowed improvement of therapeutic index of cytotoxic drugs (such as antineoplastics, antibiotics) or sustained drug release and reduction of the frequency of administration of analgesics and local anesthetics, and potentiate the immunogenicity of vaccines against hepatitis A and influenza. Furthermore, the performances of the marketed pharmaceuticals which represent pulmonary surfactant substituents (in the form of liposome vesicles) in premature infants and topical preparations with high molecular weight actives (e.g., heparin sodium) encapsulated in liposomes, were highlighted. The most important factors that affect the development of new drugs with this type of nanomaterials and their safety were commented.