The effective encapsulation of antitumor drugs by dynamic host–guest interactions at the submicromolar level remains a challenge.Herein,we report a cleavable self-inclusion camptothecin-cucurbit[7]uril(CPT-CB[7])conj...The effective encapsulation of antitumor drugs by dynamic host–guest interactions at the submicromolar level remains a challenge.Herein,we report a cleavable self-inclusion camptothecin-cucurbit[7]uril(CPT-CB[7])conjugate.The binding affinity of CB[7]to CPT is greatly enhanced owing to the intramolecular self-inclusion,demonstrating a concentrationindependent encapsulation efficiency of nearly 100%.The disulfide linker of CPT-CB[7]conjugate can be cleaved in the reductive tumor microenvironment,transforming the self-inclusion into a binary host–guest complexation pattern,thus releasing the CPT thoroughly.The enhanced biocompatibility and antitumor bioactivity of the cleavable self-inclusion conjugate have been confirmed by in vitro and in vivo experiments.This line of research will open new horizons for supramolecular drug delivery systems operating in diluted and competitive conditions.展开更多
基金supported by the Ministry of Science and Technology of China(grant no.2018YFA0208900)the National Natural Science Foundation of China(grant no.21821001)the Strategic Priority Research Program of Chinese Academy of Sciences(grant no.XDB36000000).
文摘The effective encapsulation of antitumor drugs by dynamic host–guest interactions at the submicromolar level remains a challenge.Herein,we report a cleavable self-inclusion camptothecin-cucurbit[7]uril(CPT-CB[7])conjugate.The binding affinity of CB[7]to CPT is greatly enhanced owing to the intramolecular self-inclusion,demonstrating a concentrationindependent encapsulation efficiency of nearly 100%.The disulfide linker of CPT-CB[7]conjugate can be cleaved in the reductive tumor microenvironment,transforming the self-inclusion into a binary host–guest complexation pattern,thus releasing the CPT thoroughly.The enhanced biocompatibility and antitumor bioactivity of the cleavable self-inclusion conjugate have been confirmed by in vitro and in vivo experiments.This line of research will open new horizons for supramolecular drug delivery systems operating in diluted and competitive conditions.
