Polymer-Based Prodrugs for Cancer Chemotherapy

Chemotherapy has achieved great success in cancer treatment during recent past decades, but it is still challenged by poor solubility, low tumor selectivity, and associated toxicity of most anticancer drugs. The prodrug strategy is one of the most commonly used chemical/biochemical strategies towards improving the therapeutic index of anticancer drugs. A prodrug is defined as a chemically modified drug derivative that is inactive or less active but metabolized in vivo to release the parent active component in the pharmacological environment to improve the drug’s desirability, including water solubility, patient acceptability (e.g. decreasing pain on injection), and pharmacokinetics (absorption, biodistribution, metabolism, and elimination; ADME). A typical prodrug normally consists of three parts (Figure 11.1): (1) the parent drug exerting therapeutic effects; (2) the chemical linker bridging the parent drug and the modifier; and (3) the modifier endowing the prodrug with