Abstract

Natural phenolic compounds are known not only for their multiple bioactivities but also for their low bioavailability and rapid metabolism in the systemic circulation. It is well-known that grafting these phenolic compounds to bio-based polymers such as hyaluronic acid (HA), has the advantage to increase their stability and water solubility. HA has CD44 receptors that are overexpressed on cancer cells. This makes from HA an interesting vector for antitumor drug delivery systems. The work reported herein describes the synthesis and the structural characterization of HA/vanillin conjugates as well as the size and shape of their aqueous microassemblies using dynamic light scattering and scattering electron microscopy. Finally, investigation on the bioactivity of such conjugates demonstrates that grafting vanillin to HA improves significantly its cytotoxicity against MDA-MB231 cancer cells in both dose and time-dependent manner, and reduces the migration ability as well as the number and the volume of breast cancer spheres.

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