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Abstract: Transformations of the difunctionalizated cyclodextrin derivatives is a daunting task due to the challenging purification and unambiguous characterization of the final compounds. Lactose has the ability to recognize the liver cells, and the folate receptor (alpha subunit) is overexpressed in multiple tumors, including liver cancer. Therefore, cyclodextrin conjugated with lactose and folic acid should have the liver cell targeting capability, and its inclusion complex with liver cancer drug such as Sorafenib, not only can increase drug ‘s water solubility but also increase the drug’s targeting ability. Fondaparinux as a synthetic heparin may improve the survival of cancer patients, so lactose and Fondaparinux conjugated cyclodextrin derivative can increase drug’s solubility and drug’s anti-tumor efficacy. Accordingly, Fondaparinux, folic acid and lactose conjugated 6A,6D-bifunctionlized -cyclodextrin derivatives are designed and synthesized as potential liver cancer drug carriers in order to increase cancer drug’s targeting ability, solubility and stability.