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As one of the most promising and effective delivery systems for targeted controlled-release drugs, nanocarriers (NCs) have been widely studied. Although the development of nanoparticle preparations is very prosperous, the safety and effectiveness of NCs are not guaranteed and cannot be precisely controlled due to the unclear processes of absorption, distribution, metabolism, and excretion (ADME), as well as the drug release mechanism of NCs in the body. Thus, the approval of NCs for clinical use is extremely rare. This paper reviews the