Abstract: Based on the feature of tumors reduction-responsive milieu, a novel type of glutathione (GSH)-responsive polyprodrug amphiphiles, PCPTM-b-PEG-b-PCPTM triblock copolymers was fabricated, with CPT loading content higher than 50% (mass fraction). It is found that aqueous self-assembly of PCPTM-b-PEG-b-PCPTM is strongly dependent on common solvent compositions, affording two kinds of distinct nanostructures, staggered lamellae and large compound micelles determined by TEM and SEM analysis with the common solvent to be 1,4-dioxane and DMF, respectively. Further cellular experiments reveal that both staggered lamellae and large compound micelles possess relatively high rates of tumor cellular internalization and effective anticancer performance.

Key words: polyprodrug amphiphile, self-assembly, reduction-response, nanostructure, anticancer