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Graphical Abstract:

Background: Colorectal cancer (CRC) is the third most common cancer in the world. 5-Fluorouracil (5-FU) is a conventional and most effective drug used in the clinic for the treatment ofCRC. However, the clinical use of 5-FU is limited due to the acquired resistance and systemictoxicity, such as hepatotoxicity and gastrointestinal toxicity. Objective: Recent advances in nanomedicine are being exploited to develop nanoparticle platformsto overcome resistance and therapeutic delivery of active molecules. Here, we developed 5-FUloaded sulfadiazine-poly(lactide-co-glycolide) nanoparticles (SUL-PLGA NPs) to be applied in thecolorectal cancer model. Methods: We assessed the in vivo efficacy of the SUL-PLGA NPs to enhance the antitumor effectof 5-FU. Results: In vivo treatment with 5-FU-SUL-PLGA NPs significantly reduced tumor growth in acolon cancer xenograft model compared to free 5-FU and 5-FU loaded non-targeted NPs. Treatmentwith 5-FU-SUL-PLGA NPs also increased blood vessel diameters within tumors, whichcould act in conjunction to enhance antitumor efficacy. In addition, 5-FU-SUL-PLGA NPs significantlyreduced liver mass and lung mass, which are the most common metastasis sites of CRC, anddecreased liver hepatotoxicity compared to free 5-FU drug and 5-FU loaded non-targeted NPs. Conclusion: Our findings suggest that the use of 5-FU-SUL-PLGA NPs is a promising strategy toenhance 5-FU efficacy against CRC.