Nowadays, formulation research utilizes multidisciplinary approaches to effectively deliver drugs to targeted site, regulating metabolomics, pharmacokinetics, toxicity, immunogenicity, and biometrics. Drug delivery technology was originated in 1952, and the first generation of drug delivery systems (DDSs) significantly promoted the development of oral and transdermal drugs, while the second generation attempted to achieve the smart DDSs. However, the third generation of DDSs is expected to overcome physicochemical and biological obstacles to achieve targeted drug delivery using various novel technologies, such as the pulsatile release DDSs and feedback-regulated DDSs. Subsequently, the integration of biology and biomedical materials science led to the development of biomaterials. Besides, advanced knowledge about the human body and its properties, as well as the occurring of the concept of biocompatibility, provides a theoretical basis to design and take advantage of biomaterials as DDSs. Thus, the development of new DDSs plays a critical role in the treatment of various diseases.