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Pharmaceuticals

Self-Assembly Gives Anticancer Drug An Edge

Camptothecin conjugated to a peptide self-assembles into nanomaterials that kill cancer cells effectively

by Stu Borman
March 4, 2013 | A version of this story appeared in Volume 91, Issue 9

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Credit: Adapted from JACS
The hydrophobic anticancer drug camptothecin couples with hydrophilic peptides to form amphiphiles that self-assemble into nanostructures for drug delivery.
Cui and coworkers use a linker to combine the hydrophobic cancer drug camptothecin with a hydrophilic peptide. The resulting conjugate self-assembles into nanostructures that can be used for drug delivery.
Credit: Adapted from JACS
The hydrophobic anticancer drug camptothecin couples with hydrophilic peptides to form amphiphiles that self-assemble into nanostructures for drug delivery.

An anticancer drug conjugate has been shown to self-assemble into nanostructures that can be administered directly to cancer cells and kill them, without the need for additional carriers or delivery vehicles. The approach could enable drugs to release over time at higher levels and with less toxicity than previously possible. Honggang Cui and coworkers at Johns Hopkins University show that hydrophilic peptides conjugated with different numbers of units of the hydrophobic anticancer drug camptothecin form amphiphiles that self-assemble into nanotubes and nanofibers. The nanomaterials release camptothecin inside cancer cells, wiping out cancer in vitro (J. Am. Chem. Soc., DOI: 10.1021/ja3115983). In 2010, Youqing Shen of China’s Zhejiang University and the University of Wyoming and coworkers also showed that cancer drugs combined with nonpeptide hydrophilic agents form amphiphiles that self-assemble into nanoparticles and nanocapsules (J. Am. Chem. Soc., DOI: 10.1021/ja909475m). Both groups’ nanostructures carry higher drug loads and potentially have less long-term toxicity than synthetic drug carriers such as micelles, liposomes, polymer particles and vesicles, and gold nanoparticles.

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