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HA-NPs-PTC209 is an orally active nanomedicine designed to target colorectal cancer (CRC) by reversing tumor stemness. The system consists of nanoparticles loaded with PTC209, a small molecule inhibitor of the Polycomb group protein BMI-1, which are surface-modified with hyaluronic acid (HA). The HA modification serves as a targeting ligand with high affinity for CD44 and CD168 receptors, which are frequently overexpressed on CRC cells and cancer stem cells. By delivering PTC209 directly to the tumor site via oral administration, the formulation inhibits BMI-1 expression, thereby reversing the stemness of CRC cells, inhibiting tumor growth, and preventing metastasis to the gastrointestinal system. This delivery approach aims to provide a sustained release profile while minimizing the systemic side effects and discomfort associated with traditional intravenous chemotherapy.
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