The present invention belongs to the field of nano biomedicine technology, and is especially one kind of amphiphilic chitosan cystamine grafted derivative and its preparation and application. The structural formula of the amphiphilic chitosan cystamine grafted derivative is shown as a formula (1), and the details of substituent groups are shown in the specification. Said invention is high in reaction efficiency, simple and easy to implement, and its required equipment and raw material are easily available. Studies have shown that the nanomicelles prepared with amphiphilic chitosan cystamine grafted derivatives have good biocompatibility, and show high entrapment capacity and redox-responsive release behavior of antitumor drugs. Carriers with good application value. Formula (1).
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