The objective of the study is to prepare the nano particles of 5-fluorouracil with targeted delivery to the colon with enhancement of bioavailability and decrease the side effects of the drug. 5-Fluorouracilloaded PLGA nanoparticles were developed by double solvent evaporation technique method. Characterization was carried out by determination of encapsulation efficiency (%), loss on Drying. The in-vitro drug release of drug 5- Fluorouracil was carried out for formulations (F1-F4), it is concluded that F4 was the best formulation which shows the most desired rate drug release and concluded that the polymer PLGA have a capacity of protection the drug in the GI and small intestinal Fluid hence, the maximum release of drug in the colonic region of large intestine. (c) 2021 Elsevier Ltd. All rights reserved. Selection and peer-review under responsibility of the scientific committee of the Symposium on Synthesis, Characterization & Processing of Inorganic, bio and nano Materials -2021.