Bicellar mixtures have been used as alignable membrane substrates for the structural characterization of membrane-associated proteins. Most recently, it has been shown that bicelles can serve as nanocarriers to effectively deliver hydrophobic molecules to cancer cells with a 3- to 10-fold enhancement compared to that of chemically identical liposomes. In this chapter, a detailed preparation protocol, common structural characterization methods, the structural stability and the cellular uptake of bicellar nanodisks are discussed.