Novel biotin-linked amphiphilic calix[4]arene-based supramolecular micelles as doxorubicin carriers for boosted anticancer activity

Supramolecular carrier-mediated chemotherapy is a highly attractive strategy for targeted drug delivery. In this study, four novel biotin-linked calix[4]arenes BPCA1-BPCA4 have been rationally designed to construct nano-complex with doxorubicin. The in vitro and in vivo assessments reveal that BPCA4-DOX with excellent stability are capable of affording significantly superior anti-tumor activity and lower side effects. The lack of targeting, severe toxicity on normal tissues have become an intractable limitation of doxorubicin (DOX)-based chemotherapy. A biotin-modified calix[4]arene based therapeutic agent BPCA4 has been designed for the delivery of DOX to alleviate the adverse side effects.