Abstract: Plant polyprenols were a class of natural compound of esters with good biological activity, such as anticancer, hepatoprotective and antiviral. However, the strong hydrophobic of polyprenols resulted in the low bioavailability in the human body. In view of the structural characteristics of plant polyprenols containing multiple unconjugated double bonds and terminal hydroxyl groups, the research progress of polyprenols chemical modifications, such as addition, oxidation, esterification, amination, alkylation and grignard reaction were summarized, and a series of representative polyprenols derivatives and their biological activities were introduced. Meanwhile, the latest design and development of nanoemulsions, liposomes and injections based on plant polyprenols and their derivatives were reviewed, which provide a reference for further research into the development of pharmaceutical drugs of polyprenols and their derivatives.