(309) A Two-component Two-step Transformable Nanoplatform against Cancers Based on Bioorthogonal Chemistry
Introduction: To achieve higher drug targeting and efficacy against cancers, a two-component two-step (TCTS) delivery approach is proposed (Fig 1A). In the first step, a peptide-based nanoparticle was administered, and transformed into nanofibers[1] on binding to the cancer cells. In the second step, when all the nanoparticles in the normal organs were eliminated, the tetrazine-prodrug was administered. Owing to the highly efficient bioorthogonal click reaction, the tetrazine-drug was selectively captured by the nanofibers carrying TCO (trans-cyclooctene) [2, 3] at tumor sites to achieve tumor targeting.
Learning Objectives:
Synthesize, prepare, and characterize the transformable nanoparticles and the tetrazine-CBZ prodrugs
Demonstrate the nanofibrillar transformation and bioorthogonal click chemistry in vitro and in vivo
Evaluate the anticancer efficacy of the two-component two-step drug delivery system
