Boron clusters as broadband membrane carriers

Abstract The membrane translocation of hydrophilic substances constitutes a challenge for their application as therapeutic compounds and labelling probes 1–4 . To remedy this, charged amphiphilic molecules have been classically used as carriers 3,5 . However, such amphiphilic carriers may cause aggregation and non-specific membrane lysis 6,7 . Here we show that globular dodecaborate clusters, and prominently B 12 Br 12 2− , can function as anionic inorganic membrane carriers for a broad range of hydrophilic cargo molecules (with molecular mass of 146–4,500 Da). We show that cationic and neutral peptides, amino acids, neurotransmitters, vitamins, antibiotics and drugs can be carried across liposomal membranes. Mechanistic transport studies reveal that the carrier activity is related to the superchaotropic nature of these cluster anions 8–12 . We demonstrate that B 12 Br 12 2− affects cytosolic uptake of different small bioactive molecules, including the antineoplastic monomethyl auristatin F, the proteolysis targeting chimera dBET1 and the phalloidin toxin, which has been successfully delivered in living cells for cytoskeleton labelling. We anticipate the broad and distinct delivery spectrum of our superchaotropic carriers to be the starting point of conceptually distinct cell-biological, neurobiological, physiological and pharmaceutical studies.