The Self-Assembly of Anticancer Camptothecin-Dipeptide Nanotubes: A Minimalistic and High Drug Loading Approach to Increased Efficacy

20‐(S)‐Camptothecin (CPT)‐conjugated dipeptides are reported that preassemble into nanotubes with diameters ranging from 80–120 nm. These nanoassemblies maintain a high (∼47 %) drug loading and exhibit greater drug stability (i.e., resistance to lactone hydrolysis), and consequently greater efficacy against several human cancer cells (HT‐29, A549, H460, and H23) in vitro compared with the clinically used prodrug irinotecan. A key and defining feature of this system is the use of the CPT‐conjugated dipeptide as both the drug and precursor to the nanostructured carrier, which simplifies the overall fabrication process. Happy campers: Camptothecin (CPT)‐conjugated dipeptides self‐assemble into nanotube delivery vehicles with high drug loading levels. These nanostructures display greater hydrolytic stability and greater efficacy against several human cancer cells (HT29, A549, H460, and H23) in vitro compared with the clinically used prodrug irinotecan.