Abstract: OBJECTIVE To prepare and characterize the eptoposide (VP-16)-loaded D-α tocopheryl polyethylene glycol succinate (TPGS) micelles.METHODS The VP-16/TPGS was prepared using thin-film hydration method.The particle size and Zeta potential were measured.The drug release behavior,cellular uptake and cytotoxicity were also studied.At last,the hemocompatibility was also evaluated.RESULTS The prepared VP-16/TPGS micelles had small sizes,high drug loading capacity and encapsulated efficiency.The VP-16/TPGS micelles also exhibited a sustained and controllable in vitro release behavior.The enhanced cellular uptake of the VP-16/TPGS micelles by H446 celles improved the cytotoxicity.Besides,the VP-16/TPGS micelles showed a good hemocompatibility.CONCLUSION VP-16/TPGS nanomicelle may be a safe and efficient drug delivery system for VP-16.