Advanced functional two‐dimensional (2D) nanomaterials offer unique advantages in drug delivery systems for disease treatment. Kaolinite (Kaol), a nanoclay mineral, is a natural 2D nanomaterial because of its layered silicate structure with nanoscale layer spacing. Recently, Kaol nanoclay is used as a carrier for controlled drug release and improved drug dissolution owing to its advantageous properties such as surface charge, strong biocompatibility, and naturally layered structure, making it an essential development direction for nanoclay‐based drug carriers. This review outlines the main physicochemical characteristics of Kaol and the modification methods used for its application in biomedicine. The safety and biocompatibility of Kaol are addressed, and details of the application of Kaol as a drug delivery nanomaterial in antibacterial, anti‐inflammatory, and anticancer treatment are discussed. Furthermore, the challenges and prospects of Kaol‐based drug delivery nanomaterials in biomedicine are discussed. This review recommends directions for the further development of Kaol nanocarriers by improving their physicochemical properties and expanding the bioapplication range of Kaol.