Small-molecule delivery by nanoparticles for anticancer therapy

Abstract

Using nanoparticles for the delivery of small molecules in anticancer therapy is a rapidly growing area of research. The advantages of using nanoparticles for drug delivery include enhanced water solubility, tumor-specific accumulation and improved antitumor efficacy, while reducing nonspecific toxicity. Current research in this field focuses on understanding precisely how small molecules are released from nanoparticles and delivered to the targeted tumor tissues or cells, and how the unique biodistribution of the drug-carrying nanoparticles limits toxicity in major organs. Here, we discuss existing nanoparticles for the delivery of small-molecule anticancer agents and recent advances in this field.

Figure 1. The advantages of using nanoparticles for delivering small-molecule anticancer agents

(a) TNPs improve the solubility of anticancer agents; (b) TNPs enhance the circulation time of anticancer agents in the blood vessels; (c) TNPs facilitate the accumulation of anticancer agents in targeted tumor tissues; (d) the targeting features of TNPs allow drug uptake by tumor cells through endocytosis, resulting in increased intracellular drug concentrations; (e) TNPs achieve controlled and stable drug release; and (f) TNPs are not substrates for ATP-binding cassette proteins, thereby minimizing efflux pump-mediated drug-resistance.

Figure 2. Targeting metastatic cancer by TNPs

(a) TNPs could specifically block the tumor vasculature in both primary and metastatic sites by targeting tumor-associated endothelial cells; (b) TNPs could recognize cancer cells with metastatic signatures; (c) TNPs could catch and kill metastatic cancer cells in circulation; and (d) TNPs could inhibit metastatic cells by blocking the interaction between cancer cells and new microenvironments.