In 21st century, carcinoma is predicted to be a remarkable health problem. The condition of the cancer patients will be critical when it comes to its remedy by chemotherapy using artificial anticancer molecules with various chemo side effects. In the field of nanotechnology, the nanomaterials are rapidly developing. Nanomaterials become admirable and necessary in lot of areas of human interest because of their exclusive size - dependent properties, chemical reactivity, conductivity, and enlarged strength. Carbon nanotubes (CNT) are referred to as nanomaterials. In this present world of medical research and the bio sensing technology has the capability to transform the CNT in the field of efficient medicine delivery, biosensor strategies for ailment treatment and for the health tracking. Our present work is an strive to probe the loading and release of 5- Fluorouracil from Multi Walled Carbon Nanotubes (MWCNTs) to cancer tissues. MWCNTs were subjected to covalent functionalization by using the strong acids, the oxidised MWCNTs are obtained in covalent functionalization process. Through this operation, carboxy (-COOH) groups are set up at the open sides (tips) and at the defects on the sidewalls of MWCNTs and then covalent functionalized MWCNTs were loaded with 5- Fluorouracil to prepare covalent functionalized MWCNTs-5-Flourouracil conjugate. Covalent functionalized MWCNTs-5-Flourouracil conjugate were subjected for SEM studies, TEM studies, particle size, zeta potential, drug entrapment efficiency and in vitro drug release. The release of drug shows longer than 40 h from covalent functionalized MWCNTs-5-Flourouracil conjugate and thus to manage the release of drug in controlled manner. The present research work presents esteemed, novel, and easy to prepare formulation of MWCNTs with superior drug entrapment efficiency with increased hydrophilic property of MWCNTs, and thus increases the bioavailability at selected site with narrow systemic toxicity.