Synthesis of acid-activated reversible conversion supramolecular nanoplatform: application in drug delivery and anti-tumor activity

Supramolecular nanoplatforms with stimuli-responsive behavior feature sensitive performance and effective drug delivery, which are desirable as intelligent drug delivery systems. Generally, tumor cells are characterized by excessive acid production, resulting in a lower pH in the tumor microenvironment (pH < 6.5) than in normal tissues (pH ≈7.4) and providing the possibility for the drug delivery system to exploit this decrease in pH as a trigger for drug release. Here, an acid-sensitive supramolecular nanoplatform (CM-β-CD/FC12+Br− NPs) with assembly/disassembly properties was designed and constructed, which was exploited to capture, deliver, and release anti-tumor compound CSL. 2D NOESY was utilized to examine the host–guest interaction and the potential mechanism for CM-β-CD/FC12+Br− NPs loading CSL. CM-β-CD/FC12+Br− NPs present good blood compatibility. Cytotoxicity assay revealed that CSL-loaded NPs display minimal toxicity against normal cells BEAS-2B and good anticancer ability against five human cancer cell lines, especially for Human hepatoma cell line SMMC-7721. In addition, cell apoptosis and cycle assay further verified that CSL-loaded NPs-induced apoptosis in SMMC-7721 cells up to 93