A review discusses the use of SynB vectors for intracellular and brain delivery.The ability to deliver large hydrophilic mols. is a great challenge due to the bioavailability restriction imposed by the cell membrane.As rapid advances in cell and mol. biol. lead to a proliferation of potent mols. that cannot be effectively delivered to cells and brain by conventional means, continuing refinement of the new delivery methods will be essential for realizing the potential of these mol. drugs.The use of SynB vectors and other CPPs for drug delivery represents a novel and promising approach.The cell culture and animal experiments have provided evidence that SynB-conjugated cargoes can successfully transport drugs across the membranes of many different cell types, and furthermore can traverse the more demanding BBB.The approach is broadly applicable to many diseases and the insights gained during the last decade have led to the design of more efficient peptide vectors.The optimization of these vectors will also be aided by a greater understanding of the transport mechanisms operating at the cell membranes and the BBB.