The present invention relates to the field of nano biomedicine technology, and is especially one kind of amphiphilic lipoyl cationic chitosan derivative and its preparation process and application. The structural formula of the amphiphilic lipoyl cationic chitosan derivative is shown as a formula (1). Wherein R is a lipoamide-containing pyridinium salt, The average degree of polymerization n is in the range of 20-60, The steps for preparing the amphipathic compound are simple and easy to implement, and the nano micelle prepared from the amphipathic lipoyl cationic chitosan derivative has good biocompatibility, shows high entrapment capacity and redox responsive release behavior of antitumor drugs, and is a carrier with good application value. Formula (1).
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