Cancer is a rapidly growing life-threatening disease that affected 18.1 million people worldwide in 2018. Various conventional techniques like surgery, radiation, and chemotherapy are considered as a mainstream treatment for patients but show some limitations like cytotoxicity due to off-targeted action, poor intra-tumor localization, development of multi-drug resistance by tumor cells, physical and psychological stresses, etc. Such limitations have motivated the scientists to work towards more patient-centric and precision therapy using advanced drug delivery systems like liposomes, nanoparticles, nanoconjugates, etc. However, these carriers also face limitations like poor biocompatibility, lesser payload capacity, leakage of encapsulated drug, and short-term stability. So, this review article explores the profound insights for the development of biomacromolecule- functionalized nanoconjugates to potentiate the anticancer activity of therapeutic agents for various cancers like lung, colorectal, ovarian, breast and liver cancer. Researchers have shown interest in biofunctionalized nanoconjugates because of advantages like biocompatibility, site-specificity with better localization, higher entrapment with long-term stability and lesser off-target toxicity. The progressive trend of biomacromolecule nanoconjugates will encourage further research for the development of effective transport of drugs, nutraceuticals and phytoconstituents for on-site effect at cancer microenvironment and tumor cells with higher safety profile.