Targeted drug delivery is suggested to be especially amenable for the treatment of cancer. However, specific and effective cellular internalization of oligonucleotide therapeutics such as small interfering RNA (siRNA) by tumor cells is undeniably the most prominent hurdle to surmount. The challenges to maintaining systemic circulation of siRNA in mammals are already established: serum instability, low bioavailability, recognition deficit of tumoral tissues, and the toxicity related to the use of RNA interference-based formulations. This review will focus on appropriate delivery vectors with an emphasis on the use of suitable polymers for the preparation of targeted micelles complexing siRNAs. The resulting structure, physicochemical properties, and biological activities will be given with particular attention to targeting as a key component of the main in vivo achievements, deducing that these nanocarriers should be considered nonbiological complex drugs and appear to be a promising approach for the codelivery of cytostatic drugs and siRNAs looking forward.