Disclosed are a triptolide-folic acid targeted nano-drug, a preparation method therefor and the use thereof. The preparation method is as follows : (1) dissolving Mal-PEG-PLGA in a solvent to prepare a solution A; (2) dissolving mercapto-folic acid in a solvent to prepare a solution B; (3) mixing the solution A and solution B to obtain FA-PEG-PLGA; (4) dissolving the FA-PEG-PLGA in a solvent to prepare a solution C; (5) dissolving triptolide in a solvent to prepare a solution D; and (6) mixing the solution C and the solution D as an organic phase, using deionized water as an aqueous phase, reacting the organic phase with the aqueous phase under microfluidic control, and collecting the reaction solution and subjecting same to dialysis to obtain the triptolide-folic acid targeted nano-drug.