A potentially fatal illness, cancer claims the lives of millions of people worldwide. Nanomedicine is one type of medical treatment that is always becoming more and more important. Numerous nanocarriers have been developed for therapeutic purposes; however, those based on polymers are becoming more significant because of their extended blood circulation duration, biodegradability, biocompatibility, and ability to target the desired location. The present review studied several multifunctional polymeric nano-sized formulations, including superparamagnetic iron oxide nanoparticles (SPIONs), chitosan and polystyrene, poly (lactic-co-glycolic acid) (PLGA) based nanoparticles (NPs), conjugated fluorescent polymeric NPs, gadolinium NPs, gold NPs and carbon nanotubes (CNT) used in cancer theranostic. We specifically discussed how polymeric NPs have been utilized to develop nano-sized formulations for the treatment and detection of various types of malignancies using theranostic methods, followed by an explanation of how computational analysis can be used to develop cancer therapy that minimizes the adverse effects of chemotherapy by taking into consideration various biological factors and screening drug molecules virtually. Regulators' perspectives on the safety and efficacy of polymeric nanomedicines for cancer treatment, considering factors like material properties, animal studies, and clinical trial design, have also been explored. Polymer-based nanomedicines face challenges in standardization, long-term safety, and navigating regulations. Future directions involve international collaboration to improve standards and accelerate development for better patient care.