The present application discloses a highly water-soluble
paclitaxel compound chemically modified with a bisaconitic
acid molecule, a synthesis method, and applications. The compound comprises
paclitaxel and two
aconitic acid molecules covalently bonded via an
ester bond. The preparation method of the water-soluble
paclitaxel compound is simple and suitable for industrial production. The paclitaxel
drug molecule, after structural modification by the method of the present application, possesses amphiphilic properties, i.e., both hydrophilic and lipophilic properties. The improved water
solubility and permeability provide the possibility of developing various oral and
aerosol inhalation drug formulations. The compound has high water
solubility at
room temperature, dissolves without foaming, and can reach a concentration of more than 8 mg / ml without requiring any cosolvent. The compound has lower
toxicity than the original
drug paclitaxel. The
ester bond of the compound undergoes accelerated
hydrolysis and cleavage under the weakly acidic conditions of
tumor tissue in vivo, thereby exhibiting certain
tumor tissue targeting properties, good
bioavailability, and anti-tumor effects.