Chemical modification of small molecule hydrophobic drugs is a clinically proven strategy to devise prodrugs with enhanced treatment efficacy.While this prodrug strategy improves the parent drug’s water solubility and pharmacokinetic profile,it typically compromises the drug’s potency against cancer cells due to the retarded drug release rate and reduced cellular uptake efficiency.We report here the supramolecular design of self-assembling prodrugs with much improved water solubility while maintaining high potency against cancer cells.The direct use of anticancer drugs to create their own nanostructures allows for fine-tuning and optimization of the drug loading and their physicochemical properties in a precise manner through molecular engineering of the underlying prodrug building units.
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