Poly-cucurbituril host – oxaliplatin and N-Phe-KLAK as guest cargos (Poly-CB-Ox-KLAK)

The Poly-cucurbituril host – oxaliplatin and N-Phe-KLAK as guest cargos refers to a supramolecular drug delivery system rather than a single biological target. This assembly utilizes a polymeric cucurbit[n]uril (typically CB[7]) framework as a host to non-covalently encapsulate two distinct therapeutic agents: the platinum-based chemotherapeutic oxaliplatin and the pro-apoptotic peptide N-Phe-KLAK (Jeon et al., 2005, Organic & Biomolecular Chemistry; Heitmann et al., 2006, JACS). The poly-cucurbituril scaffold enhances the solubility, stability, and tumor-targeted delivery of these cargos through host-guest chemistry. Once delivered to the target cells, the encapsulated oxaliplatin exerts its cytotoxic effect by forming intra-strand DNA cross-links, which inhibit DNA replication and transcription, leading to cell cycle arrest (Graham et al., 2004, Nature Reviews Drug Discovery). Simultaneously, the N-Phe-KLAK peptide, which is anchored to the host via its N-terminal phenylalanine residue, targets and disrupts the mitochondrial membrane, inducing the release of cytochrome c and activating the intrinsic apoptotic pathway (Ellerby et al., 1999, Nature Medicine). This dual-action approach is designed to maximize therapeutic efficacy and overcome drug resistance in various cancers by hitting both nuclear and mitochondrial targets (Zhang et al., 2018, Chemical Society Reviews).

Other names

Poly-CB[7] nanomedicineOxaliplatin/KLAK supramolecular assemblyCucurbit[n]uril-based co-delivery systemSupramolecular polymer nanomedicine

The system functions as a multi-cargo delivery vehicle where the poly-cucurbituril host encapsulates oxaliplatin and N-Phe-KLAK. Oxaliplatin acts by forming DNA adducts that inhibit transcription and replication. The N-Phe-KLAK peptide disrupts mitochondrial membranes, inducing the release of cytochrome c and activating the apoptotic cascade.