The invention discloses a
triptolide derivative, a preparation method and a preparation thereof, wherein the
chemical structure of the
triptolide derivative is represented by a formula (I) defined in the specification, R represents
straight chain alkyl acyl having a
carbon atom number of 2n, and n is 2-9. The present invention discloses the preparation method of the compound, wherein
triptolide and
saturated fatty acid are subjected to an
esterification reaction to obtain the compound. According t the present invention, the hydroxyl forms the ester by bonding the
saturated fatty acid on the C14 site OH of TP so as to reduce the polarity while the
fatty acid is introduced so as to effectively enhance the fat-
solubility, the property is stable, the oxidation is not easily generated, and the
drug forming property of the TP nanometer preparation can be significantly improved; liposomes, micelles, nanoparticles,
fat emulsions and other nanometer preparations prepared from the compound of the present invention have good packing effect; and the prepared nanometer preparation has advantages of high
drug loading, high
entrapment efficiency, stable property, significant
toxicity reducing, half-life prolonging, and the like.