Cancer is the second leading cause of human death after cardiovascular disease, and the most used drugs in clinics are cytotoxic agents. However, these drugs have some inherent disadvantages, such as the risk of toxicity, low selectivity, poor solubility, and so on. To overcome these shortcomings, a variety of drug delivery strategies based on prodrugs have been developed. The application of drug delivery systems can optimize ADME properties of cytotoxic agents and improve their selectivity at the target, thereby greatly enhancing the anticancer effect in clinics. At present, it has become mainstream in drug design. This review systematically summarized the studies of prodrug- based drug delivery systems over the past five to ten years, according to four aspects, solubility, controlled release, in situ concentration, and targeting.
Keywords: Drug delivery strategy, Anticancer drugs, Prodrug design, In situ concentration, Targeted drug delivery, Cytotoxic agents.