Starch-based nanosystems are considered a talented nanocarrier for drug delivery owing to their small particle size, biodegradability, and biocompatibilities. Starch-based nanosystems showed enhancement in biological activity, solubility, entrapment efficiency, and in-vitro release of several drugs. Starch-based nanosystems are categorized into two types; starch nanocrystals and starch nanoparticles. The difference between starch nanocrystals and starch nanoparticles will be summarized. Numerous techniques are employed to formulate starch-based nanosystems including chemical and physical methods. This review summarizes the existing knowledge on; a number of techniques used to formulate starch-based nanosystems, factors affecting each technique, and the advantages of combining both physical and chemical methods on the formulation time and physicochemical properties of the starch-based nanosystems. Besides, most innovative information regarding starch-based nanosystems modification on increasing entrapment efficiency will be discussed. Furthermore, applying starch-based nanosystems as effective drug delivery nanocarriers for delivering drugs and bioactive elements to improve their bioavailability will be abridged in this review.