A Platinum(IV) ProdrugPerfluoroaryl Macrocyclic Peptide Conjugate Enhances Platinum Uptake in the Brain

Effective
delivery to the brain limits the development of novel
glioblastoma therapies. Here, we introduce conjugation between platinum­(IV)
prodrugs of cisplatin and perfluoroaryl peptide macrocycles to increase
brain uptake. We demonstrate that one such conjugate shows efficacy
against glioma stem-like cells. We investigate the pharmacokinetics
of this conjugate in mice and show that the amount of platinum in
the brain after treatment with the conjugate is 15-fold greater than
with cisplatin after 5 h.