The drug camptothecin has a wide range of antitumor effects in cancers including gastric cancer, rectal and colon cancer, liver cancer, and lung cancer. Camptothecin-based drugs inhibit topoisomerase 1 (Topo 1), leading to destruction of DNA, and are currently being used as important chemotherapeutic agents in clinical antitumor treatment. However, the main obstacle associated with cancer therapy is represented by systemic toxicity of conventional anticancer drugs and their low accumulation at the tumor site. In addition, low bioavailability, poor water solubility, and other shortcomings hinder their anticancer activity. Different from traditional pharmaceutical preparations, nanotechnology-dependent nanopharmaceutical preparations have become one of the main strategies for different countries worldwide to overcome drug development problems. In this review, we summarized the current hotspots and discussed a variety of camptothecin-based nanodrugs for cancer therapy. We hope that through this review, more efficient drug delivery systems could be designed with potential applications in clinical cancer therapy.