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To develop a nano-sized drug delivery system for cancer therapy, amphiphilic hyaluronic acid conjugates were synthesized by chemical conjugation of hydrophobic 5β-cholanic acid to the backbone of hyaluronic acid (HA). The HA conjugates could form nano-sized self-aggregates under physiological conditions (PBS, pH = 7.4, 37 °C) via the hydrophobic interaction among 5β-cholanic acids. The HA nanoparticles were spherical in shape and their sizes were in the range of 350–400 nm, depending on the degree of substitution of 5β-cholanic acid. From a cellular experiment using Cy5.5-labeled HA nanoparticles, it was demonstrated that they are efficiently taken up by SCC7 cancer cells which over-express CD44, the receptor for HA. When the Cy5.5-labeled HA nanoparticles were systemically administrated into the tail vein of tumor-bearing mice, most of the nanoparticles were found in tumor and liver sites. In …