Abstract: Serum albumin is a natural carrier for in vivo hydrophobic molecules delivery, which is characterized by non-immunogenicity and biocompatibility. Serum albumin-based nanocarriers are outstanding carriers in drug delivery due to their high drug loading capacity, minor side effects, and solid tumor targeting properties. Currently, a great number of serum albumin-based nanodrugs have been approved or are in clinical and preclinical studies. Serum albumin nanocarriers with respects to the preparation methods including desolvation, emulsification, thermal gelation, nab-technology, self-assembly, spray-drying as well as their surface-modifications, and applications in drug delivery was summarized. More and more serum albumin-based nanocarriers will be introduced into the market as the research goes on.