Heparin conjugates and methods of making and use thereof are disclosed. An illustrative heparin conjugate includes a composition wherein a bile acid is bonded to heparin through the 3-carbon of the bile acid. A spacer may be interposed between the bile acid and the heparin. Another embodiment includes a targeting moiety bonded to the heparin-bile acid conjugate through a spacer. Another illustrative heparin conjugate includes heparin covalently bonded to a sulfonated moiety, such as a naphthalene trisulfonate residue. A method of treating cancer includes administering a heparin conjugate to an individual in need thereof.