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In this study, we choose Tau to functionalize the GO surface to improve its biocompatibility. Firstly, nano-scale GO was synthesized by the modified Hummer\u2019s method and ultrasonic stripping method. The taurine-modified graphene oxide carrier (Tau-GO) was synthesized by chemical method to obtain Tau-GO that has a good dispersibility and stability in water, with a zeta potential of\u2009\u2212\u200938.8\u00a0mV and a particle size of 242\u00a0nm. Based on the encapsulation efficiency evaluation criteria, the optimal formulation was determined to combine Tau-GO and 5-FU by non-covalent bonding. The 5-FU-Tau-GO was more stable in neutral environment than in acidic environment, and with a certain PH response and sustained release effect. In vivo, we compared oral and intravenous administrations of 5-FU and 5-FU-Tau-GO, respectively, using pharmacokinetic tests and related parameters and showed that 5-FU-Tau-GO oral or intravenous administration prolongs the action time of 5-FU in the body and improves its bioavailability. In addition, the inhibition of HepG2 cells that was measured by the MTT assay, showed that the IC<jats:sub>50<\/jats:sub> value of 5-FU was 196\u2009\u00b1\u20098.73\u00a0\u03bcg\/mL, and the IC<jats:sub>50<\/jats:sub> value of 5-FU-Tau-GO was 65.2\u2009\u00b1\u20090.7\u00a0\u03bcg\/mL, indicating that 5- FU-Tau-GO is more potent against HepG2 cells and has a stronger inhibitory effect on cancer cells. The effect on cell morphology that was measured using the AO\/EB staining also showed that 5-FU-Tau-GO not only disrupted cells, but also significantly induced apoptosis compared to 5-FU. We also verified by computer aided design that Tau-GO can bind better to 5-FU than to the unmodified GO, and that the formed 5-FU-Tau-GO system is more stable, and conducive to the transfer and release of 5-FU in vivo.<\/jats:p>","DOI":"10.1186\/s11671-021-03541-y","type":"journal-article","created":{"date-parts":[[2021,5,13]],"date-time":"2021-05-13T09:02:58Z","timestamp":1620896578000},"update-policy":"https:\/\/doi.org\/10.1007\/springer_crossmark_policy","source":"Crossref","is-referenced-by-count":26,"title":["Fabrication and Characterization of Taurine Functionalized Graphene Oxide with 5-Fluorouracil as Anticancer Drug Delivery Systems"],"prefix":"10.1186","volume":"16","author":[{"given":"Hao","family":"Pan","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yanjie","family":"Yu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Li","family":"Li","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Bingmi","family":"Liu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yu","family":"Liu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"297","published-online":{"date-parts":[[2021,5,13]]},"reference":[{"issue":"3","key":"3541_CR1","first-page":"134","volume":"36","author":"E Dickens","year":"2018","unstructured":"Dickens E, Ahmed S (2018) Principles of cancer treatment by chemotherapy. 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