L-Histidine (L-His) molecules in the water-ethanol solution form a highly ordered fluorescent crystals with a tunable size and geometry based on solvent ratio and growth time. This particular assembly of L-His molecules provides hydrophobic cavities inside the crystals. Here, we demonstrate that these hydrophobic cavities arrange a proper zone to store hydrophobic small molecules such as Nile red, pyrene and β-carotene. Armed with understanding this exclusive capability of L-His fluorescent crystals, we present a natural platform with tumor targetability and site-specific release. We embed doxorubicin (DOX) in the hydrophobic cavities of L-His crystals and modified the crystal surface using covalently cross-linked hyaluronic acid (HA). HA serves as an active targeting ligand with high binding affinity to cell-membrane-bound CD44 receptors overexpressed in various cancer cells. Thus, this design principle provides a tunable mean to create natural smart carriers for site-specific delivery and controlled release of hydrophobic small molecules. These scaffolds possess a strong fluorescence, which makes them easily traceable in the tumor.  <br/>

Natural fluorescent L-histidine crystals surface-functionalized with tumor-specific self-degradable hydrogels for systemic delivery of hydrophobic small molecules

2019 Fall National Meeting

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