Although nanotechnology-driven drug delivery systems are relatively new, they are rapidly evolving since the nanomaterials are deployed as effective means of diagnosis and delivery of assorted therapeutic agents to targeted intracellular sites in a controlled release manner. Nanomedicine and nanoparticulate drug delivery systems are rapidly developing as they play crucial roles in the development of therapeutic strategies for various types of cancer and malignancy. Nevertheless, high costs, associated toxicity and production of complexities are some of the critical barriers for their applications. Green nanomedicines have continually been improved as one of the viable approaches towards tumor drug delivery, thus making a notable impact on which considerably affect cancer treatment. In this regard, the utilization of natural and renewable feedstocks as a starting point for the fabrication of nanosystems can considerably contribute to the development of green nanomedicines. Nanostructures and biopolymers derived from natural and biorenewable resources such as proteins, lipids, lignin, hyaluronic acid, starch, cellulose, gum, pectin, alginate, and chitosan play vital roles in the development of cancer nanotherapy, imaging and management. This review uncovers recent investigations on diverse nanoarchitectures fabricated from natural and renewable feedstocks for the controlled/sustained and targeted drug/gene delivery systems against cancers including an outlook on some of the scientific challenges and opportunities in this field. Various important natural biopolymers and nanomaterials for cancer nanotherapy are covered and the scientific challenges and opportunities in this field are reviewed.