One of the challenges in cancer chemotherapy is the low target to non-target ratio of therapeutic agents which incur severe adverse effect on the healthy tissues. In this regard, nanomaterials have tremendous potential for impacting cancer therapy by altering the toxicity profile of the drug. Some of the striking advantages provided by the nanocarriers mediated targeted drug delivery are relatively high build-up of drug concentration at the tumor site, improved drug content in the formulation and enhanced colloidal stability. Further, nanocarriers with tumor-specific moieties can be targeted to the cancer cell through cell surface receptors, tumor antigens and tumor vasculatures with high affinity and accuracy. Moreover, it overcomes the bottleneck of aimless drug biodistribution, undesired toxicity and heavy dosage of administration. This review discusses the recent developments in active targeting of nanomaterials for anticancer drug delivery through cancer cell surface targeting, organelle specific targeting and tumor microenvironment targeting strategies. Special emphasis has been given towards cancer cell surface and organelle specific targeting as delivery of anticancer drugs through these routes have made paradigm change in cancer management. Further, the current challenges and future prospects of nanocarriers mediated active drug targeting are also demonstrated.