Drug nanocrystals (NCs) with fascinating physicochemical properties have attracted great attention in drug delivery. High drug-loading efficiency, great structural stability, steady dissolution, and long circulation time are a few examples of these properties, which makes drug NCs an excellent formulation for efficient cancer therapy. In the last two decades, there are a lot of hydrophobic or lipophilic drugs, such as paclitaxel (PTX), camptothecin (CPT), thymectacin, busulfan, cyclosporin A, 2-devinyl-2-(1-hexyloxyethyl) pyropheophorbide (HPPH), and so on, which have been formulated into drug NCs for cancer therapy. In this review, we summarized the recent advances in drug NCs-based cancer treatment. So far, there are main three methods to synthesize drug NCs, including top-down, bottom-up, and combination methods. The characterization methods of drug NCs were also elaborated. Furthermore, the applications and mechanisms of drug NCs were introduced by their administration routes. At the end, we gave a brief conclusion and discussed the future perspectives of drug NCs in cancer therapy. This article is categorized under: Implantable Materials and Surgical Technologies > Nanomaterials and Implants Therapeutic Approaches and Drug Discovery > Nanomedicine for Oncologic Disease Nanotechnology Approaches to Biology > Nanoscale Systems in Biology.
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