Objective: To study the cytotxicity and cellular uptake of CD44 receptor targeting paclitaxel-hyaluronic acid-octadecyl (PTX-HA-C18) and folate and CD44 receptors dual targeting PTX-folate-HA-C18 (PTX-FA-HA-C18) micelles. Method: Cytotoxicity and cellular uptake in vitro of Taxol and PTX-loaded micelles were performed using folate and CD44 receptors over expressing MCF-7 cell. Result: PTX-loaded HA micelles exhibited higher cytotoxicity compared with Taxol at lower PTX concentration. The cellular inhibition of FA-HA-C18 micelle was more obvious than that by HA-C18 micelle. HA micelles possessed high cellular uptake capacity

and the cellular uptake was concentration and time-dependent. FA-HA-C18 micelles exhibited higher cellular uptake compared with HA-C18 micelles. Conclusion: HA micelles has good tumor targeting ability

and FA-HA-C18 micelle exhibits excellent tumor targeting efficiency.