Abstract

Significance Nanotechnology-based drug delivery is expected to bring new hope for cancer treatment by enhancing anticancer drug efficacy, overcoming drug resistance, and reducing drug toxicity. In this respect, we developed an innovative drug delivery system based on a self-assembling amphiphilic dendrimer, which can generate supramolecular nanomicelles with large void space in their core to encapsulate anticancer drugs with high loading capacity. The resulting drug-encapsulated nanomicelles can effectively enhance drug potency and combat drug resistance by promoting cellular uptake and decreasing efflux of the anticancer drug. Moreover, this drug delivery system can significantly reduce the systemic toxicity of the free drug. The present study illustrates a successful example of how advances in dendrimer nanotechnology can be advantageously implemented to foster therapeutic perspectives.