Aptamers are RNA or DNA oligonucleotides interacting to form unique 3D target conformations with high affinity and specificity, and are emerging as a powerful class of ligands for therapeutic applications. In addition, dendrimers are well-defined nano-sized symmetric polymeric molecules. In this review, we provide an analysis of the use of dendrimers modified with aptamers as nonviral vectors to specifically target tumor cells. Various anticancer agents have been encapsulated with dendrimers complexing with aptamers, including epirubicin, camptothecin, Bcl-xL short hairpin (sh)RNA, and 5-fluorouracil rhodamine-labeled dextran. Other types of polymeric nanoparticle (NP)–aptamer bioconjugates have also been developed and loaded with Pt(IV) derivatives, to target specific tumor cells.