Active pharmaceutics could be encapsulated and released via drug delivery systems for biomedical applications. Conventional drug delivery technologies such as capsules, tablets, ointments, syrups, granules, etc., are challenging to accomplish sustained release and accurately target the specific location. In this chapter, the advanced drug delivery systems, including micelles, hydrogels, dendrimers, nanosponges, nanoemulsion, nanoparticles, liposomes, nanosphere/microspheres, and aptamer, are discussed. In particular, the designing of a controlled and sustained drug delivery system is emphasized. Furthermore, the strategies based on active and passive drug delivery, intravenous and extraneous drug delivery, are summarized. Various types of drug delivery technologies are introduced, including oral drug delivery, nasal drug delivery, rectal drug delivery, ocular drug delivery, vaginal drug delivery, and so on. In conclusion, future outlooks of advanced drug delivery systems and technologies, to facilitate the designing of new-generation drug formulations are also explored.