Antisense technology provides outstanding promise for treatment of human disease, having broad applicability and high specificity. Although advances have been made in antisense oligonucleotide chemistry, leading to increased plasma and cellular stability, and decreased toxicity, considerable potential remains for the enhancement of oligonucleotide uptake for targeted delivery of oligonucleotides. One promising avenue for achieving this is via linkage of antisense oligonucleotides to peptide carriers. This review looks at the current status of developments in this area.