RNA interference (RNAi) has been named as "breakthrough technology" in 2002 by Science magazine. In a short timespan this technology has conquered life sciences and numerous therapeutic approaches and is now well underway to become an important pilier of novel class of RNA based therapeutics. This mini-review focuses on nanomedicinal delivery approaches for siRNA that have shown promise with small molecules, and have recently been applied with the aim to deliver siRNA to humans for treatment of disease.