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The current study focuses on the preparation and optimization of lipid PLGA hybrid nanoparticles of 5-fluorouracil (5-FU-LPHNs) using a three-factor, three-level Box-Behnken design for sustained release and enhanced in-vitro anticancer efficacy. The morphology of the developed 5-FU-LPHNs was spherical and found in the range of 155.7–316.4 nm, entrapment efficiency (80%–92%), polydispersity index (0.11–0.19) and zeta potential (−19.7 mV to −29.4 mV) depicting nano-sized and stable nanoparticles. The XRD and DSC investigations showed the absence of characteristic peaks of 5-fluorouracil in the developed formulations indicating amorphization and successful encapsulation of 5-fluorouracil in the developed LPHNs. The in-vitro release showed a biphasic release pattern with an initial burst release pursued by sustained release up to 72 h. The in-vitro cytotoxicity studies of the developed 5-FU-LPHNs were found more cytotoxic than the free drug solution in HT-29 and HCT116 cancer cell lines. In both cell lines, the half maximal inhibitory concentration (IC50) values of 5-FU-LPHNs were approximately 2.06-fold and 1.83-fold, less than that of the 5-FU solution (p <.05). These results suggest that the developed LPHNs can be used as a potential drug delivery approach for the effective delivery of 5-fluorouracil with enhanced anticancer efficacy to colorectal tumors. [ABSTRACT FROM AUTHOR]