RNA interference (RNAi), as a new technology of gene therapy, has been used in the studies of many diseases in vitro, however, targeting delivery of small interference RNA (siRNA) is still a bottleneck for clinical therapy of siRNA agents.  Aptamer is a group of oligonucleotides with high affinity and targeting, and is becoming another important means of delivery for siRNA.  In this review, we summarized siRNA delivery obstacles in vivo and recent attractive developments in creatively using cell-internalizing aptamers to deliver siRNAs to target cells.